Synthesis of unsymmetric phosphorotrithioates by sequential coupling of 1,1-dichloro-,-diethylphosphanamine with thiols and sulfenyl chloride.

Herein, we present the first, one-step, direct synthesis of unsymmetric phosphorotrithioates through a process involving sequential coupling of 1,1-dichloro-,-diethylphosphanamine with thiols and sulfenyl chloride. This method showcases excellent functional group tolerance, substrate compatibility, and mild reaction conditions, offering a streamlined approach for the challenging phosphorotrithioate synthesis. Additionally, the applicability of this method can be extended to the synthesis of mixed phosphoroselenodithioates.

An efficient synthesis of 4-phenoxy-quinazoline, 2-phenoxy-quinoxaline, and 2-phenoxy-pyridine derivatives using aryne chemistry.

Herein we report the mild and efficient synthesis of 4-phenoxyquinazoline, 2-phenoxyquinoxaline, and 2-phenoxypyridine derivatives from the starting materials quinazolin-4(3)-one, quinoxalin-2(1)-one, and pyridin-2(1)-one and aryne generated from 2-(trimethylsilyl)phenyl trifluoromethanesulfonate and cesium fluoride. This synthetic methodology gives a new environmentally benign way for the preparation of several unnatural series of 4-phenoxyquinazoline, 2-phenoxyquinoxaline and 2-phenoxypyridine compounds with high yields and broad substrate scope.

Malononitrile-activated synthesis and anti-cholinesterase activity of styrylquinoxalin-2(1)-ones.

Herein, we report a base-free malononitrile activated condensation of 3-methylquinoxaline-2(1)-one (3MQ) 1 with aryl aldehydes 3a-3ad for synthesis of styrylquinoxalin-2(1)-ones (SQs) 4a-4ad with excellent yields. In this reaction, malononitrile activates the aldehyde Knoevenagel condensation towards reaction with 3MQ 1 and gets liberated during the course of reaction to yield the desired SQs 4a-4ad. The SQs were evaluated for cholinesterase inhibition and 4n was found to display a mixed type of inhibition of AChE, which was supported by molecular modelling studies.