A one-step, multi-component reaction for the synthesis of fully substituted 5-amino-4-carboxamidthiazoles

A novel multi-component reaction has been developed for the synthesis of fully substituted 5-amino-4-carboxamidthiazoles. Condensation of an aldehyde with commercially available 2-amino-2-cyanoacetamide in the presence of elemental sulfur and base affords these heterocycles in a one-pot reaction sequence. A variety of aryl, heteroaryl, and aliphatic aldehydes were successfully utilized, thus providing rapid access to functionalized thiazoles that are valuable intermediates in the synthesis of pharmacologically active compounds.