Base-promoted in situ generation of methyl acrylate from dimethyl 3, 3'-dithiodipropionate. Application To N-alkylation of heterocycles

J Org Chem. 2000 May 19;65(10):3123-5. doi: 10.1021/jo9919207.

Abstract

In basic medium, dimethyl 3,3'-dithiopropionate generates methyl acrylate, which serves in situ as a source of propionate moiety. This property was applied to the alkylation of indoles and other nitrogen heterocycles leading to a series of 3-(heteroaryl-substituted) propionates. A mechanistic rationale for the generation of acrylate is presented along with supportive experimental data.