The enantioselective construction of trifluoromethylated quaternary stereocenters via the Rh-catalyzed asymmetric dehydrated arylation of unprotected hemiaminals,Organic Chemistry Frontiers

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The enantioselective construction of trifluoromethylated quaternary stereocenters via the Rh-catalyzed asymmetric dehydrated arylation of unprotected hemiaminals
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2019/11/28 , DOI: 10.1039/c9qo01203f
Yu-Tuo Sun _{1,

2,

3,

4,

5} , Dong-Xing Zhu _{1,

2,

3,

4,

5} , Xiaofeng Rao _{6,

7,

8,

9} , Ming-Hua Xu _{1,

2,

3,

4,

5}

Affiliation

A method for the highly enantioselective Rh-catalyzed dehydrated arylation of unprotected hemiaminals has been developed, and provided a series of chiral benzosultams bearing trifluoromethylated quaternary stereocenters in high yields with excellent enantioselectivities (up to 99% ee). The synthetic utility was further demonstrated by the facile enantioselective construction of a HIV-1 inhibitor molecule.

中文翻译：

通过Rh催化的未保护的半缩醛的不对称脱水芳基化反应，对三氟甲基化的立体立体中心的对映选择性结构

已开发出一种用于未保护的半缩醛的高对映选择性Rh催化的脱水芳基化的方法，并提供了一系列具有高对映体选择性（最高99％ee）的带有三氟甲基化四级立体中心的手性苯并阿舒他姆。通过HIV-1抑制剂分子的容易的对映选择性构建进一步证明了该合成用途。

更新日期：2020-02-13

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