Enantioselective synthesis of beta-aryl-gamma-amino acid derivatives via Cu-catalyzed asymmetric 1,4-reductions of gamma-phthalimido-substituted alpha,beta-unsaturated carboxylic acid esters |
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Authors: | Deng Jun Hu Xiang-Ping Huang Jia-Di Yu Sai-Bo Wang Dao-Yong Duan Zheng-Chao Zheng Zhuo |
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Institution: | Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China. |
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Abstract: | A series of chiral beta-aryl-substituted gamma-amino butyric acid derivatives were synthesized in good enantioselectivities via the Cu-catalyzed asymmetric conjugate reduction of gamma-phthalimido-alpha,beta-unsaturated carboxylic acid esters using Cu(OAc)2 x H2O as a catalyst precursor, (S)-BINAP as a ligand, PMHS as a hydride source, and t-BuOH as an additive. The methodology has been applied successfully to the enantioselective synthesis of a chiral pharmaceutical, (R)-baclofen. |
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