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Enantioselective Michael Addition Reactions to Construct SCF3‐containing Stereocenter Catalyzed by Chiral Quaternary Phosphonium Salts
Advanced Synthesis & Catalysis ( IF 5.4 ) Pub Date : 2020-10-26 , DOI: 10.1002/adsc.202001026
Haoran Hong 1 , Changwu Zheng 2 , Gang Zhao 3 , Yongjia Shang 1
Affiliation  

The trifluoromethylthio group is significant in drug design for its high stability, electronegativity, and lipophilicity. Herein, a series of indenone structures containing the SCF3 group and an adjacent chiral quaternary stereocenter were synthesized by an asymmetric Michael addition reaction using an ion pair catalyst derived from amino acids. The desired products were obtained in excellent yields (up to 98%) and good to high stereoselectivities (up to 97% ee and >20:1 dr).

中文翻译:

手性季Ph盐催化的对映选择性迈克尔加成反应构建含SCF3的立体中心

三氟甲硫基由于其高稳定性,电负性和亲脂性而在药物设计中具有重要意义。本文中,使用衍生自氨基酸的离子对催化剂通过不对称迈克尔加成反应合成了包含SCF 3基团和相邻的手性四元立体中心的一系列茚满酮结构。以优异的收率(高达98%)和良好至高的立体选择性(高达97%ee和> 20:1 dr)获得所需产物。
更新日期:2020-12-22
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