Palladium-catalyzed one-pot synthesis of 2-alkyl-2-arylcyanoacetates |
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| Authors: | Wang Xiang Guram Anil Bunel Emilio Cao Guo-Qiang Allen Jennifer R Faul Margaret M |
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| Institution: | Chemical Process R&D, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, USA. xiangw@amgen.com |
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| Abstract: | A one-pot procedure for the synthesis of 2-alkyl-2-arylcyanoacetates based on a Pd(OAc)2/DPPF (DPPF = 1,1'-diphenylphosphino ferreocene)-catalyzed enolate arylation followed by in situ alkylation has been developed. This procedure tolerates a diverse range of aryl and heteroaryl bromides, and provides a rapid entry to a variety of 2-alkyl-2-arylcyanoacetates in good to excellent yield. |
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