Asymmetric Synthesis of CF3- and Indole-Containing Thiochromanes via a Squaramide-Catalyzed Michael-Aldol Reaction.
Asymmetric Synthesis of CF3- and Indole-Containing Thiochromanes via a Squaramide-Catalyzed Michael-Aldol Reaction.
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DOI：
10.1021/acs.orglett.6b01498
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发表时间：
2016-07
期刊：
影响因子：
5.2
通讯作者：
Yuan-Yuan Zhu-Yuan;Zhenghao Dong;Xin Cheng;Xiaoling Zhong;Xiaolin Liu;Li Lin;Zhiqiang Shen;Peiju Yang-Peiju
中科院分区：
文献类型：
--
作者：
Yuan-Yuan Zhu-Yuan;Zhenghao Dong;Xin Cheng;Xiaoling Zhong;Xiaolin Liu;Li Lin;Zhiqiang Shen;Peiju Yang-Peiju
在方酰胺催化下，β-吲哚-β-CF 3烯酮与2-巯基苯甲醛发生了Michael-Aldol反应。该方法以优异的产率、非对映选择性和对映选择性提供了一系列具有含CF 3的季立体中心的2-CF 3 -2-吲哚取代的硫代苯并二氢吡喃。
A Michael-aldol reaction of 2-mercaptobenzaldehyde with β-indole-β-CF3 enones catalyzed by a squaramide has been realized. The method affords a series of 2-CF3-2-indole-substituted thiochromanes featuring a CF3-containing quaternary stereocenter in excellent yields, diastereoselectivities, and enantioselectivities.