Clarifying the relationship and analyzing the influential factors of bronchial asthma in children with attention-deficit hyperactivity disorder.

BACKGROUND: Bronchial asthma is closely related to the occurrence of attention-deficit hyperactivity disorder (ADHD) in children, which can easily have adverse effects on children's learning and social interactions. Studies have shown that childhood asthma can increase the risk of ADHD and the core symptoms of ADHD. Compared with children with ADHD alone, children with asthma and ADHD are more likely to show high levels of hyperactivity, hyperactive-impulsive and other externalizing behaviors and anxiety in clinical practice and have more symptoms of somatization and emotional internalization. AIM: To explore the relationship between ADHD in children and bronchial asthma and to analyze its influencing factors. METHODS: This retrospective cohort study was conducted at Dongying People's Hospital from September 2018 to August 2023. Children diagnosed with ADHD at this hospital were selected as the ADHD group, while healthy children without ADHD who underwent physical examinations during the same period served as the control group. Clinical and parental data were collected for all participating children, and multivariate logistic regression analysis was employed to identify risk factors for comorbid asthma in children with ADHD. RESULTS: Significant differences were detected between the ADHD group and the control group in terms of family history of asthma and allergic diseases, maternal complications during pregnancy, maternal use of asthma and allergy medications during pregnancy, maternal anxiety and depression during pregnancy, and parental relationship status (P < 0.05). Out of the 183 children in the ADHD group, 25 had comorbid asthma, resulting in a comorbidity rate of 13.66% (25/183), compared to the comorbidity rate of 2.91% (16/549) among the 549 children in the control group. The difference in the asthma comorbidity rate between the two groups was statistically significant (P < 0.05). The results of the multivariate logistic regression analysis indicated that family history of asthma and allergic diseases, maternal complications during pregnancy, maternal use of asthma and allergy medications during pregnancy, maternal anxiety and depression during pregnancy, and parental relationship status are independent risk factors increasing the risk of comorbid asthma in children with ADHD (P < 0.05). CONCLUSION: Children with ADHD were more likely to have comorbid asthma than healthy control children were. A family history of asthma, adverse maternal factors during pregnancy, and parental relationship status were identified as risk factors influencing the comorbidity of asthma in children with ADHD. Clinically, targeted interventions based on these factors can be implemented to reduce the risk of comorbid asthma. This information is relevant for results sections of abstracts in scientific articles.

Safety and effectiveness of lurasidone in the treatment of Chinese schizophrenia patients: An interim analysis of post-marketing surveillance.

BACKGROUND: Schizophrenia is a psychiatric disorder characterized by chronic or recurrent symptoms. Lurasidone was licensed in China in 2019 for the treatment of adult schizophrenia in adults with a maximum dose of 80 mg/d. However, post-market surveillance (PMS) with an adequate sample size is required for further validation of the drug's safety profile and effectiveness. AIM: To conduct PMS in real-world clinical settings and evaluate the safety and effectiveness of lurasidone in the Chinese population. METHODS: A prospective, multicenter, open-label, 12-wk surveillance was conducted in mainland China. All patients with schizophrenia from 10 sites who had begun medication with lurasidone between September 2019 and August 2022 were eligible for enrollment. Safety assessments included adverse events (AEs), adverse drug reactions (ADRs), extrapyramidal symptoms (EPS), akathisia, use of EPS drugs, weight gain, and laboratory values as metabolic parameters and the QTc interval. The effectiveness was assessed using the brief psychiatric rating scale (BPRS) from baseline to the end of treatment. RESULTS: A total of 965 patients were enrolled in the full analysis set and 894 in the safety set in this interim analysis. The average daily dose was 61.7 ± 19.08 mg (mean ± SD) during the treatment. AEs and ADRs were experienced by 101 patients (11.3%) and 78 patients (8.7%), respectively, which were mostly mild. EPS occurred in 25 individuals with a 2.8% incidence, including akathisia in 20 individuals (2.2%). Moreover, 59 patients received drugs for treating EPS during the treatment, with an incidence of 6.6% which dropped to 5.4% at the end of the treatment. The average weight change was 0.20 ± 2.36 kg (P = 0.01687) with 0.8% of patients showing a weight gain of ≥ 7% at week 12 compared with that at the baseline. The mean values of metabolic parameters and the QTc interval at baseline and week 12 were within normal ranges. The mean changes in total BPRS scores were -8.9 ± 9.76 (n = 959), -13.5 ± 12.29 (n = 959), and -16.8 ± 13.97 (n = 959) after 2/4, 6/8, and 12 wk, respectively (P < 0.001 for each visit compared with the baseline) using the last-observation-carried-forward method. CONCLUSION: The interim analysis of the PMS of adult patients with schizophrenia demonstrate the safety and effectiveness of lurasidone in the Chinese population. No new safety or efficacy concerns were identified.

Empagliflozin ameliorates atherosclerosis via regulating the intestinal flora.

BACKGROUND AND AIMS: Sodium-glucose cotransporter 2 inhibitor (SGLT2i) has been reported to attenuate atherosclerosis. Further, it has been suggested that intestinal flora influences atherosclerosis progression. Herein we aimed to investigate whether SGLT2i can alleviate atherosclerosis through intestinal flora. METHODS: Six-week-old male ApoE-/- mice fed a high-fat diet were gavaged either empagliflozin (SGLT2i group, n = 9) or saline (Ctrl group, n = 6) for 12 weeks. Feces were collected from both groups at the end of the experiment for fecal microbiota transplantation (FMT). Another 12 six-week-old male ApoE-/- mice were fed a high-fat diet and received FMT with feces either from SGLT2i (FMT-SGLT2i group, n = 6) or from Ctrl (FMT-Ctrl group, n = 6) groups. Blood, tissue, and fecal samples were collected for subsequent analyses. RESULTS: In comparison with Ctrl group, atherosclerosis was less severe in the SGLT2i group (p < 0.0001), and the richness of probiotic, such as f_Coriobacteriaceae, f_S24-7, f_Lachnospiraceae, and f_Adlercreutzia, was higher in feces. Besides, empagliflozin resulted in a significant reduction in the inflammatory response and altered intestinal flora metabolism. Interestingly, compared with FMT-Ctrl, FMT-SGLT2i also showed a reduction in atherosclerosis and systemic inflammatory response, as well as changes in the component of intestinal flora and pertinent metabolites similar to SGLT2i group. CONCLUSIONS: Empagliflozin seems to mitigate atherosclerosis partly by regulating intestinal microbiota, and this anti-atherosclerotic effect can be transferred through intestinal flora transplantation.

Label-free detection of DNA methylation by surface-enhanced Raman spectroscopy using zirconium-modified silver nanoparticles.

DNA methylation is an important feature of gene epigenetics that affects the metabolic process of organisms. Although surface-enhanced Raman spectroscopy (SERS) has demonstrated great potential in label-free DNA detection, discriminating the various processes involved in DNA methylation remains a challenge. DNA molecules fold themselves, wrapping the hydrophobic bases, thus making it difficult for traditional methods to detect single-base signals. In this study, we develop a SERS platform for detecting DNA via modifying silver nanoparticles by zirconium ions to obtain the DNA fingerprint information of base methylations (N6-methylated adenine and 5-methylated cytosine). Zirconium ions open the folded DNA molecules, enabling SERS signals of the four DNA bases (A, C, G, T) to be obtained as well as identification of the subtle differences between normal and methylated DNA with single base-level sensitivity. Moreover, the identifying information of DNA methylation was obtained by combining principal component analysis (PCA) with 2D correlation spectroscopy analysis. The findings of this study provide a substantial progress for current platforms for DNA sequencing, genetic testing, and gene-disease treatment.

Nomogram for predicting an individual prospective hemorrhage risk in untreated brainstem cavernous malformations.

OBJECTIVE: In this study, the authors aimed to create a nomogram for precisely predicting the 5-year prospective hemorrhage risk in brainstem cavernous malformations (BSCMs). METHODS: Patients with confirmed BSCMs in a single-center prospective observational series from January 2012 to December 2016 were included in the present study for nomogram building and validation. The concordance index (C-index), calibration curves, and decision curve analysis were used to evaluate the predictive accuracy, discriminative ability, and clinical usefulness of the nomogram. Then, a nomogram-based risk stratification model for untreated BSCMs was developed. RESULTS: In total, 600 patients were included in the study; 417 patients who had been enrolled before July 2015 were divided into the training and validation cohorts, and 183 subsequently enrolled patients were used as the external validation cohort. By applying a backward stepwise procedure in the multivariable Cox model, variables, including prior hemorrhage (HR 1.69), hemorrhage on admission (HR 3.33), lesion size > 1.5 cm (HR 1.84), lesion depth (HR 2.35), crossing the axial midpoint (HR 1.94), and developmental venous anomaly (HR 2.62), were incorporated to develop a nomogram. The Harrell C-index values for a 5-year prospective hemorrhage were 0.752 (95% CI 0.687-0.816), 0.801 (95% CI 0.665-0.936), and 0.758 (95% CI 0.674-0.842) in the training, internal validation, and external validation cohorts, respectively. The nomogram performed well in terms of consistency between prediction and actual observation according to the calibration curve. The patients could be classified into three distinct (low, medium, and high) risk groups using the final score of this nomogram. CONCLUSIONS: Independent predictors of the 5-year hemorrhage risk in untreated BSCMs were selected to create the first nomogram for predicting individual prospective hemorrhage. The nomogram was able to stratify patients into different risk groups and assist in clinical decision-making.

Five-year symptomatic hemorrhage risk of untreated brainstem cavernous malformations in a prospective cohort.

Hemorrhage of brainstem cavernous malformation (CM) would cause various symptoms and severe disability. The study aimed to elaborate on the 5-year actuarial cumulative hazard of symptomatic hemorrhage. Patients diagnosed in our institute between 2009 and 2013 were prospectively registered. All clinical data were obtained, follow-up was performed, and risk factors were evaluated. Four hundred sixty-eight patients (217 female, 46.4%) were included in the study with a median follow-up duration of 79.0 months. A total of 137 prospective hemorrhages occurred in 107 patients (22.9%) during 1854.0 patient-years. Multivariate Cox analysis found age ≥ 55 years (hazard ratio (HR) 2.166, p = 0.002), DVA (HR 1.576, p = 0.026), superficial-seated location (HR 1.530, p = 0.047), and hemorrhage on admission (HR 2.419, p = 0.026) as independent risk factors for hemorrhage. The 5-year cumulative hazard of hemorrhage was 30.8% for the overall cohort, 47.8% for 60 patients with age ≥ 55 years, 43.7% for 146 patients with DVA, 37.9% for 272 patients with superficial-seated lesions, and 37.2% for 341 patients with hemorrhage on admission. As a stratified analysis, within subcohort of 341 patients with a hemorrhagic presentation, age ≥ 55 years (HR 3.005, p < 0.001), DVA (HR 1.801, p = 0.010), and superficial-seated location (HR 2.276, p = 0.001) remained independently significant. The 5-year cumulative hazard of hemorrhage was 52.0% for 119 patients with both DVA and hemorrhagic presentation. The 5-year cumulative hemorrhagic risk was 30.8% and was higher in subgroups if harboring risk factors that helped to predict potential hemorrhagic candidates and were useful for treatment decision-making.Clinical Trial Registration-URL: http://www.chictr.org.cn Unique identifier: ChiCTR-POC-17011575.

[Effect of Fang's scalp acupuncture on perceived stress and sleep structure in insomnia patients: a randomized controlled trial].

OBJECTIVE: To compare the efficacy on insomnia between Fang 's scalp acupuncture combined with conventional acupuncture and the simple conventional acupuncture. METHODS: A total of 66 patients with insomnia were randomly divided into an observation group (33 cases, 1 case dropped off) and a control group (33 cases, 2 cases dropped off). In the control group, the routine acupuncture therapy was applied to Shenmen (HT 7), Baihui (GV 20), Zhaohai (KI 6) and Sanyinjiao (SP 6), etc. Based on the treatment as the control group, Fang's scalp acupuncture therapy was supplemented at fuxiang tou, fuzang shangjiao, fuzang zhongjiao, siwei, etc. At these scalp points, the needles were inserted perpendicularly with flying needling technique and manipulated with trembling one. In either group, the treatment was given once daily, continuously for 2 weeks. Before and after treatment, separately, the score of Pittsburgh sleep quality index (PSQI) and the score of Chinese perceived stress scale (CPSS) were observed, as well as the parameters monitored by polysomnography, i.g. total sleep time (TST), sleep onset latency (SOL), wakefulness after the sleep onset (WASO), sleep efficiency (SE), the percentages of the time of rapid eye movement sleep phase (REM) and non-rapid eye movement sleep phase 1, 2, 3 and 4 in TST (REM%, N1%, N2%, N3%). The efficacy was compared between two groups. RESULTS: After treatment, the scores of each factor and the total scores of PSQI, as well as CPSS scores were all lower than those before treatment in the two groups (P<0.01, P<0.05); except the score for sleep quality, the score of each factor and the total score of PSQI, as well as CPSS score in the observation group were lower than those in the control group (P<0.01, P<0.05). After treatment, TST, SE%, REM% and N3% were increased and SOL, WASO, N1% were decreased as compared with before treatment in the two groups (P<0.01, P<0.05), and N2% in the observation group was decreased (P<0.01); SE%, REM% and N3% in the observation group were higher than the control group (P<0.05) and N1% and N2% were lower than the control group (P<0.05). The total effective rate was 93.8% (30/32) in the observation group, higher than 87.1% (27/31) in the control group (P<0.05). CONCLUSION: Fang 's scalp acupuncture, on the base of routine acupuncture, obviously improves the sleep quality and perceived stress and adjusts the sleep structure in the patients with insomnia.

Welan gum promoted the growth of rice seedlings by enhancing carbon and nitrogen assimilation.

Based on the characteristics of natural polysaccharides in film-forming, chelating, and environmental friendly, a natural polysaccharide fertilizer agent was selected to increase the utilization of nitrogen fertilizer and increase plant growth. Five polysaccharides: xanthan gum, guar gum, fenugreek gum, welan gum and chitosan were screened for plant growth promoting effect. The results showed that welan gum had the most significant effect on promoting the growth of rice seedlings, and the concentrations of 0.1 mg mL-1 and 0.15 mg mL-1 showed the best growth effects. The effects of welan gum on nitrogen utilization in rice seedlings were investigated. Results showed welan gum increased the contents of ammonium, nitrate, free amino acids, and proteins in rice seedlings. There were four key enzymes of nitrogen metabolism which are nitrate reductase, glutamine synthetase, glutamate synthase, and glutamate dehydrogenase significantly enhanced by welan gum though up-regulating the transcriptional levels of these enzymes. Therefore, nitrogen uptake and nitrogen metabolism in rice seedlings were promoted to increase the biomass of rice seedlings. Based on the research, results showed that welan gum could constitute a promising fertilizer in the future.

Adverse Factors of Treatment Response and Overall Survival in Pediatric and Adult Patients with Pineoblastoma.

OBJECTIVE: Intracranial pineoblastomas are rare neoplasms with poor prognosis. The aim of this study was to describe the independent prognostic factors and treatment strategies for overall survival in pediatric and adult patients. METHODS: Sixty-four patients were surgically treated between January 2012 and December 2018. RESULTS: The series included 37 (57.8%) males and 27 (42.2%) females. Gross total resection was achieved in 41 (64.1%) cases, and the 1-, 3-, and 5-year rates of overall survival were 86.3, 52.3, and 36.6%, respectively. In the pediatric group (n=42), 28 patients (66.7%) were male, with the median, and the mean age was 4 and 6.2±4.7 years, respectively. After a median follow-up of 25.0 months, twenty-six patients (61.9%) died, and the 1-, 3-, and 5-year rates of overall survival were 84.9, 46.4, and 26.7%, respectively. Postoperative radiotherapy (p=0.058) and postoperative chemotherapy (p=0.183) had a positive influence on the increased overall survival. Meanwhile, postoperative radiotherapy combined with chemotherapy following surgery had a positive impact on overall survival (p=0.174, Log rank). In the adult group, the mean overall survival was 67.3±9.3 months (range, 0.8-95.3 months), and the 1-, 3-, and 5-year rates of overall survival were 89.5, 64.4, and 64.4%, respectively. In this group, no statistical association was observed between clinical factors and outcomes. However, patients who received postoperative radiotherapy (60.7 vs 57.6 month, mean survival; p=0.510, Log rank) or chemotherapy (63.0 vs 59.9 month, mean survival; p=0.404, Log rank) had better survival rates compared with those who declined. CONCLUSION: In the pediatric group, surgery with postoperative radiotherapy and chemotherapy was a favorable factor for overall survival. In the adult group, a positive trend in overall survival was found when patients received radiation and/or chemotherapy following surgery.

Coumarin-3-formylpyrazoles as 3-carbon synthons in cyclocondensation for the synthesis of spiro-fused pentacyclic spirooxindoles.

Coumarin-3-formylpyrazoles have been synthesized and applied as 3-carbon synthons in reaction with 3-hydroxyoxindoles by using DABCO as the catalyst. A range of structurally diverse spiro-fused pentacyclic spirooxindoles, bearing a spirooxindole-γ-lactone and a 3,4-dihydrocoumarin substructure, could be smoothly obtained in good to excellent yields (up to 99%) with excellent diastereoselectivities (all cases >20 : 1 dr). The asymmetric version of this tandem reaction was preliminarily investigated by using chiral organocatalysts.

Organocatalytic Asymmetric Dearomatization of 3-Nitroindoles and 3-Nitrobenzothiophenes via Thiol-Triggered Diastereo- and Enantioselective Double Michael Addition Reaction.

Organocatalytic asymmetric dearomatization of 3-nitroindoles and 3-nitrobenzothiophenes by reaction with ethyl 4-mercapto-2-butenoate has been developed. A range of chiral tetrahydrothiopheneindolines and tetrahydrothiophenebenzothiophenes bearing three contiguous stereocenters are obtained in high yields with good diastereoselectivities and excellent enantioselectivities. This is the first example of thiol-triggered catalytic asymmetric dearomatization of 3-nitroindoles and 3-nitrobenzothiophenes.

Phosphine-catalyzed dearomative (3 + 2) annulation of 2-nitrobenzofurans and nitrobenzothiophenes with allenoates.

An efficient Ph2PMe-catalyzed dearomative (3 + 2) annulation of 2-nitrobenzofurans, 2-nitrobenzothiophenes, and 3-nitrobenzothiophenes with allenoates has been developed. With the developed protocol, a series of structurally important cyclopenta[b]benzofurans and cyclopenta[b]benzothiophenes were obtained in good to excellent yields (up to 98%) under mild conditions. In addition, preparative-scale experiments and transformations were conducted to exemplify the synthetic utility. The asymmetric version of this dearomative (3 + 2) annulation reaction was tentatively investigated by using chiral phosphine catalysts.

Chiral Bifunctional Amine-Squaramide-Catalyzed Highly Diastereo- and Enantioselective Michael/Aldol Cascade Reaction of 2-Mercaptobenzaldehyde and α,ß-Unsaturated 7-Azaindoline Amides.

A highly diastereo- and enantioselective Michael/aldol cascade reaction of 2-mercaptobenzaldehyde and α,ß-unsaturated 7-azaindoline amides has been developed. Using as low as 1 mol % cinchonidine-derived bifunctional squaramide as the catalyst, a range of enantioenriched thiochromenes containing three contiguous stereogenic centers were smoothly obtained in excellent results (all cases >20:1 dr, 88-99% yield and ≥99% ee). The 7-azaindoline moiety of α,ß-unsaturated 7-azaindoline amides has been demonstrated to be vital for the high reactivity and excellent stereoselectivity.

[Effect of electroacupuncture on neurological deficit and activity of TLR2/NF-κB signaling in ce-rebral ischemia /reperfusion injury rats].

OBJECTIVE: To observe the effect of electroacupuncture (EA) on neurological behavior and activity of Toll-like receptor 2 / nuclear factor kappa B (TLR2/NF-κB) signaling of the ischemic cerebral area in cerebral ischemia-reperfusion injury (CIRI) rats, so as to explore its mechanisms underlying improvement of CIRI. METHODS: A total of 120 male SD rats were randomly divided into blank control, sham operation, model, EA and EA＋NF-κB inhibitor (Pyrrolidine Dithiocarbamate Hydrochloride, PDTC, EA＋PDTC) groups which were further divided into 3, 7, 14 and 28 d subgroups (n＝6 in each subgroup). The CIRI model was established by occlusion of the middle cerebral artery for 90 min, followed by reperfusion. EA (1－20 Hz, 6 V) was applied to "Shuigou" (GV26), "Neiguan" (PC6), "Sanyinjiao" (SP6) and "Weizhong" (BL40) for 30 min, once a day for 28 days. For rats of the EA＋PDTC group, PDTC solution (120 mg/kg) was intraperitoneally injected on the 3rd day after successful modeling and before EA intervention. The neurological deficit severity (Zea Longa score) was assessed 3, 7, 14 and 28 days after modeling. The expression levels of TLR2, Interleukin-1 receptor-associated kinase (IRAK) and NF-κB mRNAs in the ischemic penumbra region of brain tissue were detected by real-time fluorescence quantitative PCR. RESULTS: Following modeling, the neurological deficit scores were significantly increased from the 3rd day on after CIRI (P<0.05), the expression levels of TLR2 mRNA on day 3, 7, 14 and 28, and IRAK mRNA on day 3 and 7, as well as NF-κB mRNA on day 3, 7 and 14 were significantly up-regulated in the model group relevant to the blank control group (P<0.05). After EA intervention, the neurological deficit scores were significantly decreased in the EA group on day 3, 7 and 28 and in the EA＋PDTC group on day 3, 7, 14 and 28 in comparison with those of the model group (P<0.05). In addition, the expression levels of TLR2 mRNA and NF-κB mRNA on day 3, 7 and 14 in the EA group, and on day 3, 7, 14 and 28 in the EA＋PDTC group, IRAK mRNA on day 3 in the EA and EA＋PDTC group were significantly down-regulated (P<0.05), but those of IRAK mRNA on day 14 and 28 in the EA group were significantly up-regulated in comparison with those of the model group (P<0.05). The effect of the EA＋PDTC was obviously superior to that of simple EA in down-regulating the expression of TLR2 (on day 28), and IRAK (on day 3, 14, 28), and NF-κB (on day 3, 7 and 14) (all P<0.05). CONCLUSION: EA stimulation can improve the symptoms of neurological deficits in CIRI rats, which may be related to its effect in suppressing the expression of TLR2, NF-κB and IRAK mRNAs of the ischemic cerebral tissue, i．e., down-regulating the activity of TLR2/NF-κB signaling.

Organocatalyzed Asymmetric Dearomative Aza-Michael/Michael Addition Cascade of 2-Nitrobenzofurans and 2-Nitrobenzothiophenes with 2-Aminochalcones.

An organocatalyzed dearomative aza-Michael/Michael addition cascade of 2-nitrobenzofurans and 2-nitrobenzothiophenes with 2-aminochalcones has been developed, opening a new channel to access a series of optically active tetrahydrobenzofuro[3,2- b]quinolines and tetrahydrobenzo[4,5]thieno[3,2- b]quinolines bearing three contiguous stereocenters with excellent diastereo- and enantioselectivities (all cases >20:1 dr, up to 99% ee). This study features the first asymmetric dearomative cascade reaction of 2-nitrobenzofurans and 2-nitrobenzothiophenes beginning with aza-Michael addition. The potential applications of the methodology were demonstrated by the preparative-scale experiment and the versatile transformations of the products.

Missense mutation in PRKCQ is associated with Crohn's disease.

OBJECTIVE: Recent genome-wide association studies have demonstrated that rs2236379 in PRKCQ is a novel significant locus for Crohn's disease (CD). However, the association has not been replicated in any populations. We therefore aimed to investigate the prevalence of the PRKCQ rs2236379 variant in the Chinese Han population and evaluate whether the genetic variant of PRKCQ confers susceptibility to CD and is associated with its clinical characteristics. METHODS: A total of 283 patients with CD and 381 healthy controls were enrolled. Genomic DNA was extracted from their whole blood samples and polymerase chain reaction-restriction fragment length polymorphism was used for genotyping. The association between PRKCQ polymorphisms and susceptibility to CD, and between genotypes and clinical phenotypes was analyzed. RESULTS: A higher frequency of the T allele was discovered in CD patients than in healthy controls (P = 0.027). A significant difference in the distribution of the TT and CT/CC genotypes was observed between CD patients and controls (P = 0.024). The TT genotype showed a significant association with susceptibility to CD (odds ratio 1.647, 95% confidence interval: 1.088-2.574, P = 0.019). Patients with CD with the rs2236379 TT mutant risk genotype were most likely to exhibit perianal disease (P = 0.044). CONCLUSIONS: Our research revealed an association between the PRKCQ rs2236379 (C>T) and CD. The TT homozygous mutation increased the risk of developing CD and may contribute to perianal disease.

Organocatalyzed Dearomative Cycloaddition of 2-Nitrobenzofurans and Isatin-Derived Morita-Baylis-Hillman Carbonates: Highly Stereoselective Construction of Cyclopenta[ b]benzofuran Scaffolds.

The first organocatalyzed asymmetric dearomative cycloaddition between 2-nitrobenzofurans and isatin-derived Morita-Baylis-Hillman carbonates has been developed. Using a modified cinchona alkaloid as the catalyst, a series of structurally diverse cyclopenta[ b]benzofuran derivatives with three contiguous stereocenters, including a spiro-quaternary chiral center, could be smoothly obtained in excellent results (all cases >20:1 dr, up to 99% yield and 98% ee). The utility of this method was showcased by the versatile transformations of the product.

Facile synthesis of fused polycyclic compounds via intramolecular oxidative cyclization/aromatization of ß-tetralone or ß-tetralone oximes.

A mild and efficient NBS promoted intramolecular oxidative cyclization/aromatization of ß-tetralone oximes has been explored. Under the optimized conditions, fused α-carbolines containing pentacyclic rings were obtained in moderate to good yields. Furthermore, various benzo[5,6]chromeno[2,3-b]indoles were successfully synthesized in moderate yields from ß-tetralones using slightly modified conditions. We proposed a possible reaction pathway based on the experimental results.

Synthesis of polycyclic spirooxindoles via an asymmetric catalytic one-pot stepwise Aldol/chloroetherification/aromatization procedure.

A general method for the synthesis of chiral pentacyclic spirooxindoles containing a tetrahydropyrano[2,3-b]indole scaffold through a one-pot stepwise sequence from 3-(3-indolomethyl)oxindole, paraformaldehyde and NCS is reported. Furthermore, the pentacyclic spirooxindoles could be transformed to bispirooxindole and other structurally diverse spirocyclic oxindoles.