Alkynyl Cinchona Catalysts affect Enantioselective Trifluoromethylation for Efavirenz under Metal-Free Conditions

作者：Okusu Satoshi; Hirano Kazuki; Yasuda Yoshimasa; Tanaka Junki; Tokunaga Etsuko; Fukaya Haruhiko; Shibata Norio^*

来源：Organic Letters, 2016, 18(21): 5568-5571.

DOI：10.1021/acs.orglett.6b02807

Efavirenz is manufactured worldwide, and its asymmetric synthesis requires a complex organometallic approach, while an organocatalytic approach is far less efficient. The first highly enantioselective approach is disclosed for the synthesis of Efavirenz under nonmetal organocatalysis with up to 93% ee for the Merck intermediate and 91% ee for the Lonsa intermediate using novel alkynyl cinchona catalysts.

• 出版日期2016-11-4