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Design, synthesis and anti-HIV-1 activity of 4,6-dibenzyl-2-oxo-1,2-dihydropyridine-3-carbonitrile

A-Min Li, Xiang-Yi Liu, Xiao-Wei Wang*, Jun-Yi Liu*   

  1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2011-05-19 Revised:2011-07-20 Online:2011-09-20 Published:2011-09-20
  • Contact: Xiao-Wei Wang*, Jun-Yi Liu*

Abstract:

An effective synthesis method for preparing 4,6-disubstituted pyridinones was reported. Ethyl 3-oxo-4-phenylbutyrate was an important intermediate, by which 6-substituted pyridinones could be prepared. The decarboxylation condition was optimized for compound 4. After protected with a methoxy group, the compound was reacted with BnBr to form the target compound 11. The structures were characterized by 1H NMR, 13C NMR and HRMS, and its enzyme inhibition activity was also determined.

Key words: HIV-1, NNRTIs, Pyridinone analogues, Decarboxylation

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