A Serendipitous One-Pot Cyanation/Hydrolysis/Enamide Formation: Direct Access to 3-Methyleneisoindolin-1-ones

A direct, one-pot conversion of 2'-haloacetophenones to 3-methyleneisoindolin-1-one scaffolds using CuCN as the sole reagent without the need for moisture-free or anaerobic conditions is reported. This serendipitously discovered transformation with a broad substrate scope provides a significantly different route towards these important scaffolds. The scope of the method has also been further extended towards the synthesis of three special scaffolds, which are analogous to various bio-active drugs.

Automated summary

The research presents a method using CuCN to directly convert 2'-haloacetophenones into 3-methyleneisoindolin-1-one scaffolds, with a broad substrate scope. It also demonstrates the potential of this method in synthesizing three special scaffolds analogous to various bio-active drugs.