Enantioselective Mannich‐Type Reactions to Construct Trifluoromethylthio‐Containing Tetrasubstituted Carbon Stereocenters via Asymmetric Dual‐Reagent Catalysis
Enantioselective Mannich‐Type Reactions to Construct Trifluoromethylthio‐Containing Tetrasubstituted Carbon Stereocenters via Asymmetric Dual‐Reagent Catalysis
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DOI：
10.1002/adsc.201700321
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发表时间：
2017-09
影响因子：
5.4
通讯作者：
Lijun Xu;Hongyu Wang;Changwu Zheng;Gang Zhao
中科院分区：
文献类型：
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作者：
Lijun Xu;Hongyu Wang;Changwu Zheng;Gang Zhao
通过不对称有机膦催化的Mannich型反应，实现了同时具有SCF 3基团和氰基的四取代碳立构中心的构建。以高产率和中至高对映选择性获得产物。可以从每个反应中分离出两种非对映异构体（总共25个实施例），使得这种方法成为产生分子多样性和改善相关候选药物的生物活性的可行机会。
The approach to construct the tetrasubstituted carbon stereocenter bearing both a SCF3 group and a cyano group has been realized, through asymmetric organophosphine-catalyzed Mannich-type reactions. The products were obtained with high yields and moderate to high enantioselecitivities. Two diastereomers could be isolated from each reaction (25 overall examples), rendering this approach a viable opportunity for molecular diversity generation and improvement of the bioactivity of related drug candidates.