Synergistic Visible Light and Pd-Catalyzed C-H Alkylation of 1-Naphthylamines with α-Diazoesters.

The combination of visible light irradiation and Pd-catalysis has been practically employed for the C-H alkylation reactions of naphthylamines and α-diazo esters, leading to the synthesis of α-naphthyl functionalized acetates via C-C bond construction under mild reaction conditions and under solvent-free conditions. The light irradiation has been proven to play a pivotal role in the reactions, probably by promoting the generation of active carbene species from α-diazo esters.

Thiazole-5-carbaldehyde Synthesis by Cascade Annulation of Enaminones and KSCN with Dess-Martin Periodinane Reagent.

The Dess-Martin periodinane (DMP) reagent-mediated reactions of tertiary enaminones with potassium thiocyanate for the synthesis of thiazole-5-carbaldehydes are developed. The product formation involves cascade hydroxyl thiocyanation of the C═C double bond, intramolecular hydroamination of the C≡N bond, and thiazole annulation by condensation on the ketone carbonyl site, representing novel reaction pathways in the reactions between enaminones and thiocyanate salt. DMP plays dual roles in mediating the free radical thiocyanation and inducing the unconventional selective thiazole-5-carbaldehyde formation by masking the in situ generated formyl group during the reaction process.

The Effects of High-Intensity Interval Training on Exercise Capacity and Prognosis in Heart Failure and Coronary Artery Disease: A Systematic Review and Meta-Analysis.

Objective: The purpose of this study is to compare the effects of high-intensity interval training (HIIT) versus moderate-intensity continuous training (MICT) on exercise capacity and several prognostic markers in patients with coronary artery disease (CAD) and heart failure (HF). Methods: This systematic review is registered on the INPLASY website (number: INPLASY202080112). We conducted a comprehensive search in eight databases of literature before September 13, 2019. Trials comparing HIIT and MICT in participants with CAD or HF aged 52-78 years were included. Exercise capacity (peak oxygen consumption (peak VO2)) and prognostic markers, such as the anaerobic threshold (AT), minute ventilation/carbon dioxide production (VE/VCO2) slope, left ventricular ejection fraction (LVEF), and prognostic value of the predicted VO2 max per cent (the predicted VO2 peak (%)) were examined. Results: A total of 15 studies were included comprising 664 patients, 50% of which were male, with an average age of 60.3 ± 13.2 years. For patients with CAD, HIIT significantly improved peak VO2 values (95% CI 0.7 to 2.11) compared with MICT, but peak VO2 values in patients with HF did not seem to change. For training lasting less than eight weeks, HIIT significantly improved peak VO2 values (95% CI 0.70 to 2.10), while HIIT lasting 12 weeks or longer resulted in a modestly increased peak VO2 value (95% CI 0.31 to 5.31). High-intensity interval training significantly increased the AT when compared with MICT (95% CI 0.50 to 1.48). High-intensity interval training also caused a moderate increase in LVEF (95% CI 0.55 to 5.71) but did not have a significant effect on the VE/VCO2 slope (95% CI -2.32 to 0.98) or the predicted VO2 peak (95% CI -2.54 to 9.59) compared with MICT. Conclusions: High-intensity interval training is an effective therapy for improving peak VO2 values in patients with CAD. High-intensity interval training in the early stage (eight weeks or fewer) is superior to MICT. Finally, HIIT significantly improved prognostic markers, including the AT and LVEF in patients with CAD and HF.

[Study on the biomechanical analysis and influencing factors study for the treatment of humeral epicondylitis by Bachuorounian manipulation].

OBJECTIVE: To quantitatively study the biomechanical parameters of Bachuorounian manipulation in the treatment of humeral epicondylitis, and discuss the effects of individual characteristics on the biomechanical parameters were discussed. METHODS: From July 2019 to February 2020, 40 patients with external humeral epicondylitis were selected, including 18 males and 22 females, ranging in age from 20 to 50 years old, with an average of (34.37±8.41) years old;and the course of disease ranged from 1 to 11 months, with a mean of (6.05±2.71) months. The biomechanical parameters of the elbow joint of the affected side were measured by using the biomechanical sensor. At thesame time, the individual characteristic parameters of patients were collected to analyze the influence of different individual characteristics of patients on biomechanical parameters. RESULTS: The results of mechanical analysis in each stage of the bachuorounian manipulation were as follows:the rolling back rotation force was (31.17±2.99) N;the buckling bending drawing force was (44.99±2.38) N;the rolling pre rotation force was (31.03±2.75) N;and stretching drawing force was (48.75±2.09) N. The correlation analysis between the parameters showed that there was a significant positive correlation between the buckling bending drawing force and the stretching drawing force parameters, and a significant positive correlation between the rolling force back-rotation force and the rolling pre-rotation force parameters. The multivariate linear regression analysis on the parameters of influencing factors and manipulative biomechanics showed that there was a significant correlation between body weight and rolling back-rotation force, significant correlation between elbow tenderness and the buckling bending drawing force, and significant correlation between disease duration and the stretching drawing force. CONCLUSION: The bachuorounian manipulation of humeral epicondylitis has a certain range of operating force. Manipulation of each stage has a correlation and systematic. The patient's weight, elbow tenderness and disease course are important factors affecting the bachuorounian manipulation.

Copper-Catalyzed Enaminone C(sp2)-N Bond Phosphonation for Stereoselective Synthesis of Alkenylphosphonates.

A direct enaminone C-N bond coupling functionalization that generates a new C-P bond using dialkyl phosphonate for the efficient and stereoselective synthesis of (E)-alkenylphosphonates is reported. The reactions toward target products proceed well with a broad scope, disclosing a valuable new synthetic application of enaminones by the interesting C(sp2)-N bond elaboration.

[Effect of early rehabilitation combined with abdomen needle therapy for motor function and psychological obstacle of stroke].

OBJECTIVE: To study the clinical effect of early rehabilitation combined with abdomen needle therapy for the motor function and psychological obstacle of stroke based on the western medical treatment. METHODS: Ninety patients with acute stroke were randomly divided into an observation group A,an observation group B and a control group, 30 cases in each group. Conventional western medical treatment and early rehabilitation for the affected limbs wete applied in the three groups for one month. Besides,abdomen needle therapy was used on Qihai(CV 6),Guanyuan(CV 4),Tianshu(ST 25),Daheng(SP 15),Huaroumen(ST 24),Wailing(ST 26),Shangfengshidian,Shangfengshiwaidian,Xiafengshidian and Xiafengshixiadian in the observation group A. The needles were retained for 20 min without activity of the affected limbs. Based on the treatment as the group A,early rehabilitation was adopted in the observation group B. All treatment was given once a day,and 10 times were taken as a course. Three courses were required with two days at the interval. Fugl-Meyer assessment(FMA),Hamilton anxiety scale(HAMA),Hamilton depression scale(HAMD) and China stroke scale(CSS) were used before and after treatment. RESULTS: Scores of FMA、HAMA、HAMD and CSS after treatment were improved than those before treatment in the three groups(all P<0.05). All the above scores of the two observation groups were better than those of the control group(all P<0.05). The scores of HAMA and HAMD of the observation group B were superior to those of the observation group A(both P<0.05). CONCLUSIONS: Conventional treatment combined with abdomen needle therapy can improve the motor function and the psychological obstacle of stroke,and the effect is better than that of the conventional treatment. Early rehabilitation based on the two therapeutic methods can help relieve psychological status.

Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline.

A novel series of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline were synthesized and tested for their antiproliferative activities against five human cancer cell lines including A549 (lung cancer), MCF-7 (breast adenocarcinoma), HeLa (cervical carcinoma), HT29 and HCT-116 (colorectal cancer). Most of the synthesized compounds showed broad spectrum antiproliferative activity (IC50 1.47-11.83 µM), of which 8f, 8m and 8q were the most active members with IC50 values in the range of 1.58-2.27, 1.84-3.27 and 1.47-4.68 µM against five cancer cell lines examined, respectively. Further investigations revealed that compounds 8f, 8m and 8q exhibited weak inhibition against dihydrofolate reductase and no activity against thymidylate synthase, while induced DNA damage and activated the G2/M checkpoint in HCT-116 cells.

Palladium-catalyzed Hiyama-type cross-coupling reactions of arenesulfinates with organosilanes.

Palladium-catalyzed Hiyama-type cross-coupling reactions of various arenesulfinates with organosilanes were achieved in good to excellent yields under aerobic conditions at 70 °C. Fluoride is essential, and tetrabutylammonium fluoride (TBAF) was shown to be the most efficient additive for these cross-coupling reactions. These cross-coupling reactions of the arenesulfinates provide high yields and show wide functional group tolerance, making them attractive alternative transformations to traditional cross-coupling approaches for carbon-carbon bond construction.

Pd-catalyzed C-3 functionalization of indolizines via C-H bond cleavage.

New transition metal-catalyzed methods for the arylation of indolizines by the direct cleavage of C-H bonds have been developed. A wide range of aryltrifluoroborate salts react with indolizines in the presence of Pd(OAc)(2) catalyst and AgOAc oxidant to give the arylated indolizines in high yields. Both electron-donating and electron-withdrawing groups perform smoothly while bromide and chlorine substituents are tolerated. In addition, the indolizines display similar reactivities in the Pd-catalyzed reaction with 3-phenylpropiolic acid to afford the corresponding C-3 alkynylated indolizines. These methods allow the direct functionalization of indolizines in one step.