立体中心
三氟甲基
化学
对映选择合成
替代(逻辑)
催化作用
酒
群(周期表)
分子
立体化学
药物化学
有机化学
组合化学
烷基
计算机科学
程序设计语言
作者
Guangzheng Tian,Mingtong Ji,Fan Wu,Guan Wang,Changwu Zheng,Xiaoyu Wu
出处
期刊:Organic Letters
[American Chemical Society]
日期:2023-06-22
卷期号:25 (25): 4666-4671
标识
DOI:10.1021/acs.orglett.3c01521
摘要
The trifluoromethyl group is one of the most functional and widely used fluoroalkyl groups in medicinal chemistry and drug discovery. However, few methodologies have been reported for the asymmetric introduction of the trifluoromethyl group into organic molecules. In this study, a diastereo- and enantioselective propargylic substitution reaction was performed between propargylic carbonates and 2,2,2-trifluoroethyl-substituted nitroisoxazoles catalyzed by a Cu-pybox complex. This method enables the preparation of a series of propargylation products with two contiguous stereogenic centers, one of which is a chiral trifluoromethyl-bearing carbon. In most cases, the desired products were produced in high yields with good to excellent diastereo- and enantioselectivities.
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