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Semisynthesis of CRV431.
Li, Feng-Xia; Zhang, Qing-Zhou; Li, Shi-Jun; Lin, Guang; Huo, Xiang-Yu; Lan, Yu; Yang, Zhen.
Afiliação
  • Li FX; State Key Laboratory of Chemical Oncogenomics and Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, China.
  • Zhang QZ; State Key Laboratory of Chemical Oncogenomics and Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, China.
  • Li SJ; Green Catalysis Center and College of Chemistry, Zhengzhou University, 100 Science Avenue, Zhengzhou, Henan 450001, P. R. China.
  • Lin G; State Key Laboratory of Chemical Oncogenomics and Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, China.
  • Huo XY; State Key Laboratory of Chemical Oncogenomics and Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, China.
  • Lan Y; Green Catalysis Center and College of Chemistry, Zhengzhou University, 100 Science Avenue, Zhengzhou, Henan 450001, P. R. China.
  • Yang Z; School of Chemistry and Chemical Engineering, and Chongqing Key Laboratory of Theoretical and Computational Chemistry, Chongqing University, Chongqing 400030, P. R. China.
Org Lett ; 23(9): 3421-3425, 2021 05 07.
Article em En | MEDLINE | ID: mdl-33844557
ABSTRACT
The non-immune-suppressive cyclophilin inhibitor CRV431 is a clinical candidate to cure nonalcoholic steatohepatitis (NASH) and has the potential to treat liver fibrosis and cancer incidence. Herein we report a concise chemical semisynthesis of CRV431 in four steps from the commercially available cyclosporine, featuring in this the flow-chemistry-based methylenation an intermolecular ring-closing metathesis and a Rh-catalyzed diastereoselective hydrogenation.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2021 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2021 Tipo de documento: Article