【摘 要】
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Enantioselective phosphine organocatalysis has advanced rapidly over the past decades as a powerful tool for the preparation of numerous structurally divers
【机 构】
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KeyLaboratoryofSyntheticChemistryofNaturalSubstances,ShanghaiInstituteofOrganicChemistry,ChineseAcad
【出 处】
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中国化学会第十三届全国有机合成化学学术研讨会
论文部分内容阅读
Enantioselective phosphine organocatalysis has advanced rapidly over the past decades as a powerful tool for the preparation of numerous structurally diverse compounds.Herein,we have reported a chiral amino acid-derived multifunctional organophosphine-based dual-reagent catalytic system and have successfully applied it to the asymmetric Mannich reaction and cyanation of imines.1,2 The key finding of this work is that the zwitterion intermediate,which is generated in situ by mixing a chiral multifunctional organophosphine with methyl acrylate,could serve as an efficient Bronsted or Lewis base catalyst for asymmetric synthesis.The excellent yields and enantioselectivities (up to 99% yield,up to 99% ee),very low catalyst loading (as low as 0.1 mol%),broad substrate scope,scalability,and mild reaction conditions are significant features of the reaction system.
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