Ultrasound-assisted synthesis and in vitro antimicrobial activity of novel 5-oxo-2-pyrrolidinecarboxamides and 7-oxo-2-azepanecarboxamides

摘要

A facile one-pot reaction has been set up for the synthesis of novel 5-oxo-2-pyrrolidinecarboxamides and 7-oxo-2-azepanecarboxamides 4a-j from three-component reaction of keto carboxylic acids 1a-d, various primary amines 2a-b and isocyanides 3a-b under ultrasound irradiation. The present protocol offers attractive characteristics such as easy handling methodology, good-to-excellent yields, environmental friendliness, clean reaction, higher atom economy, convenient operation, and shorter reaction time. The newly synthesized 5-oxo-2-pyrrolidinecarboxamides and 7-oxo-2-azepanecarboxamides 4a-j have been screened for their antimicrobial activity and the majority of these cyclic amides exhibited weak antimicrobial activity.