title: Alkynyl Cinchona Catalysts affect Enantioselective Trifluoromethylation for Efavirenz under Metal-Free Conditions.
abstract: 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.
authors.affiliation: Department of Nanopharmaceutical Sciences & Department of Frontier Materials, Nagoya Institute of Technology , Gokiso, Showa-ku, Nagoya, 466-8555, Japan.
authors.forename: Satoshi
authors.initials: S
authors.lastname: Okusu
authors.affiliation: Department of Nanopharmaceutical Sciences & Department of Frontier Materials, Nagoya Institute of Technology , Gokiso, Showa-ku, Nagoya, 466-8555, Japan.
authors.forename: Kazuki
authors.initials: K
authors.lastname: Hirano
authors.affiliation: Department of Nanopharmaceutical Sciences & Department of Frontier Materials, Nagoya Institute of Technology , Gokiso, Showa-ku, Nagoya, 466-8555, Japan.
authors.forename: Yoshimasa
authors.initials: Y
authors.lastname: Yasuda
authors.affiliation: Department of Nanopharmaceutical Sciences & Department of Frontier Materials, Nagoya Institute of Technology , Gokiso, Showa-ku, Nagoya, 466-8555, Japan.
authors.forename: Junki
authors.initials: J
authors.lastname: Tanaka
authors.affiliation: Department of Nanopharmaceutical Sciences & Department of Frontier Materials, Nagoya Institute of Technology , Gokiso, Showa-ku, Nagoya, 466-8555, Japan.
authors.forename: Etsuko
authors.initials: E
authors.lastname: Tokunaga
authors.affiliation: National Institute of Advanced Industrial Science and Technology (AIST) , Moriyama, Nagoya, 463-8560, Japan.
authors.forename: Haruhiko
authors.initials: H
authors.lastname: Fukaya
authors.affiliation: Department of Nanopharmaceutical Sciences & Department of Frontier Materials, Nagoya Institute of Technology , Gokiso, Showa-ku, Nagoya, 466-8555, Japan.
authors.forename: Norio
authors.initials: N
authors.lastname: Shibata