Synthesis of 3-acyl, methylene and epoxy substituted isoindolinone derivatives via the ortho-lithiation/cyclization procedures of aromatic imines with carbon monoxide

A simple and convenient one-pot synthesis of 3-acyl, methylene and epoxy isoindolinone derivatives via the reaction of o-lithiated aromatic imines with carbon monoxide followed with acyl chlorides or PhCO(CH2)(n)Br (n = 1 or 3) under mild reaction conditions has been developed. Preliminary in vitro tests for fungicidal activity of these isoindolinone derivatives indicated that most of them exhibit good fungicidal activity against Sclerotinia sclerotiorum. (C) 2017 Elsevier Ltd. All rights reserved.