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Application of Enzymatic Promiscuity in Pharmaceutical Synthesis: Papain-catalyzed One-pot Synthesis of 1,4-Dihydropyridine Calcium Channel Antagonists and Derivatives
Authors:JIANG Ling  YE Wenting  SU Weike  YU Chuanming
Affiliation:1. Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, P. R. China;
2. Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, P. R. China
Abstract:A new method for the synthesis of 1, 4-dihydropyridine (1, 4-DHP) calcium channel antagonists felodipine, nitrendipine and their derivatives via papain-catalyzed three-component reactions of aldehyde, methyl acetoacetate and ethyl 3-aminocrotonate was developed. Operational simplicity, mild reaction conditions and eco-friendliness are the key features of this protocol.
Keywords:Papain  Catalytic promiscuity  Multicomponent reaction  1  4-Dihydropyridine calcium channel antagonist  
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