Electrochemical dehydrogenative phosphorothiolation of heteroarenes

Abstract

An electrochemical dehydrogenative phosphorothiolation of heteroarenes for the synthesis of S-heteroaryl phosphorothioates has been developed. The reaction employs elemental sulfur as the S-source. By avoiding the use of transition-metal catalysts, base, external oxidants, highly toxicity and sensitivity of the reagents, a variety of S-heteroaryl phosphorothioates have been prepared. This phosphorothiolation reaction shows high functional group compatibility, and can be easily scaled-up to gram quantities.