A One-Step, Atom Economical Synthesis of Thieno[2,3-d]-pyrimidin-4-amine Derivatives by a Four-Component Reaction

摘要

A Na_2HPO_4-catalyzed four-component reaction between a ketone, malononitrile, S8 and formamide has been realized for the first time. This reaction provides a concise approach to thieno[2,3-d]pyrimidin-4-amines, previously requiring 5 steps. The utility of this reaction was validated by preparing a multi-targeted kinase inhibitor and an inhibitor of the NRF2 pathway with excellent atom- and step-economy.