Synthesis of Unsymmetrical 3,3'-Dialkyloxindole Boronic Esters from 3-Alkylidene-2-oxindoles Enabled by Copper Catalysis.

We describe a 1,2-alkylboration of 3-alkylidene-2-oxindoles with a diboron reagent and alkyl bromides and iodides enabled by copper/bisphosphine catalysis. This scalable alkylboration method provides facile access to 3,3'-dialkyloxindole boronic esters featuring an all-carbon quaternary stereocenter and an increased F(sp3) fraction. In addition to good functional group tolerance and prolific utilization of drug/pesticide-derived alkyl iodides, the conversion of the C-B bond to a C-C/C-X bond offers further opportunities for structural variation of 3,3'-dialkyloxindoles.

Active Case Finding among Adults using an Individual's Vulnerability Score for Pulmonary Tuberculosis in a Rural Village of Goa: A Cross-sectional Study.

Background: "Detect-Treat-Prevent-Build" to achieve tuberculosis (TB)-free India is envisaged in the National Tuberculosis Elimination Program (NTEP). To be able to achieve this, it is important to address the fact that the most vulnerable and hard-to-reach groups need to undertake screening. The present review aimed to examine the vulnerability in connection with TB disparities faced by distinct sub-populations generally viewed as vulnerable and follow these for testing. Materials and Methods: The community-based cross-sectional study was conducted in the field practice area of sub-center Carambolim in a rural area of Goa for 3 months. The households were visited, and data collected via personal interviews were recorded on the questionnaire study tool. Based on the data, the participants' vulnerability mapping was done per the parameters identified. Results: Among 223 households, 528 persons were screened for vulnerability. The 47 highly vulnerable participants were advised sputum CBNAAT, of which 9 (19%) tested positive for pulmonary TB, while of the 86 moderately vulnerable participants, 4 (5%) tested positive for pulmonary TB. Among the 34 with symptoms suggestive of TB, 3 (9%) tested positive for pulmonary TB. Conclusions: The study detected 16 new TB patients from the population and found a higher incidence of pulmonary TB among the vulnerable group with no symptoms of Pulmonary TB. A further state-wide survey is recommended to diagnose such cases.

Visible-Light-Photocatalyzed Dicarbofunctionalization of Conjugated Alkenes with Ketone-Based Dihydroquinazolinones.

A visible-light-photocatalyzed 1,2-arylalkylation of N-(arylsulfonyl)acrylamides with ketone-based dihydroquinazolinones is described. The formal C-C bond cleavage of aliphatic ketones is unified with tandem radical alkylation/1,4-aryl migration/desulfonylation to forge two different types of vicinal C-C bonds and construct an all-carbon quaternary α-stereocenter, thus enhancing the carbogenic complexity and tolerating diverse functionalities. Additional to telescopic synthesis and product diversification, this method features a radical dicarbofunctionalization of conjugated N-(arylsulfonyl)acrylamides with a nucleophilic alkyl radical precursor (dihydroquinazolinone) utilizing oxygen as a green oxidant at ambient temperature.

Case Report: Novel mutations in TBC1D24 are associated with autosomal dominant tonic-clonic and myoclonic epilepsy and recessive Parkinsonism, psychosis, and intellectual disability.

Mutations disrupting presynaptic protein TBC1D24 are associated with a variable neurological phenotype, including DOORS syndrome, myoclonic epilepsy, early-infantile epileptic encephalopathy, and non-syndromic hearing loss. In this report, we describe a family segregating autosomal dominant epilepsy, and a 37-year-old Caucasian female with a severe neurological phenotype including epilepsy, Parkinsonism, psychosis, visual and auditory hallucinations, gait ataxia and intellectual disability. Whole exome sequencing revealed two missense mutations in the TBC1D24 gene segregating within this family (c.1078C>T; p.Arg360Cys and c.404C>T; p.Pro135Leu). The female proband who presents with a severe neurological phenotype carries both of these mutations in a compound heterozygous state. The p.Pro135Leu variant, however, is present in the proband's mother and sibling as well, and is consistent with an autosomal dominant pattern linked to tonic-clonic and myoclonic epilepsy. In conclusion, we describe a single family in which TBC1D24 mutations cause expanded dominant and recessive phenotypes. In addition, we discuss and highlight that some variants in TBC1D24 might cause a dominant susceptibility to epilepsy.