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A one-step, atom economical synthesis of thieno[2,3-d]pyrimidin-4-amine derivatives via a four-component reaction.
Shi, Taoda; Zerio, Christopher J; Sivinski, Jared; Ambrose, Andrew J; Moore, Kohlson T; Buckley, Thomas; Kaneko, Lynn; Zhang, Mae; Zhang, Donna D; Chapman, Eli.
Afiliación
  • Shi T; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Zerio CJ; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Sivinski J; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Ambrose AJ; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Moore KT; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Buckley T; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Kaneko L; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Zhang M; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Zhang DD; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
  • Chapman E; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, 1703 East Mabel Street, P.O. Box 210207, Tucson, AZ 85721, United States.
European J Org Chem ; 20(2): 3269-3272, 2019 Jun 02.
Article en En | MEDLINE | ID: mdl-31857792
ABSTRACT
A Na2HPO4-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.
Palabras clave

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Tipo de estudio: Health_economic_evaluation Idioma: En Revista: European J Org Chem Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Tipo de estudio: Health_economic_evaluation Idioma: En Revista: European J Org Chem Año: 2019 Tipo del documento: Article País de afiliación: Estados Unidos