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Organocatalytic enantioselective indole alkylations of alpha,beta-unsaturated ketones
Authors:Chen Wei  Du Wei  Yue Lei  Li Rui  Wu Yong  Ding Li-Sheng  Chen Ying-Chun
Affiliation:Key Laboratory of Drug-Targeting of Education Ministry and Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu, 610041, China.
Abstract:The C3-selective enantioselective Michael-type Friedel-Crafts alkylations of indoles with nonchelating alpha,beta-unsaturated alkyl ketones, catalysed by a chiral primary amine derived from natural cinchonine, were investigated. The reactions, in the presence of 30 mol% catalyst, were smoothly conducted at 0 to -20 degrees C. Moderate to good ee (47-89%) has been achieved.
Keywords:
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