Ambient Temperature Metal-Free Thiomethylation of Chloroheteroarenes and Chloropurines.

Herein, we report an in-situ mild and metal-free protocol for thiomethylation of heteroarenes in high yields. The thiomethylation of various chloropurines, nucleosides, and chloroheteroarenes has been accomplished offering easy access to agrochemicals and synthetic molecules useful for drug discovery.

Ambient-Temperature, Metal-Free, CDI-Mediated Ex-Situ Conversion of Acids to Amides: A Useful Late-Stage Strategy.

An efficient ex-situ method for the amidation of carboxylic acids mediated by CDI has been disclosed herewith. This metal-free strategy is performed at ambient temperature and can be applied effectively for late-stage modification of amino acids and APIs.