A one-step, atom economical synthesis of thieno[2,3

Autor: Taoda, Shi, Christopher J, Zerio, Jared, Sivinski, Andrew J, Ambrose, Kohlson T, Moore, Thomas, Buckley, Lynn, Kaneko, Mae, Zhang, Donna D, Zhang, Eli, Chapman
Rok vydání: 2019
Předmět:
Zdroj: European J Org Chem
ISSN: 1434-193X
Popis: A Na(2)HPO(4)-catalyzed four-component reaction between a ketone, malononitrile, S(8) 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.
Databáze: OpenAIRE