CATALYTIC ENANTIOSELECTIVE MANUFACTURING METHOD OF (S)-2-(5-CHLORO-2-NITROPHENYL)-4-CYCLOPROPYL-1,1,1-TRIFLUOROBUT-3-YL-2-OL AS KEY INTERMEDIATE OF AIDS THERAPEUTIC AGENT EFAVIRENZ USING PHASE TRANSFER CATALYST DERIVED FROM 5-ETHYNYL CINCHONA ALKALOID

Title:

Document Type and Number:

Japanese Patent JP2016132632

Kind Code:

A

Abstract:

PROBLEM TO BE SOLVED: To provide a manufacturing method of (S)-2-(5-chloro-2-nitrophenyl)-4-cyclopropyl-1,1,1-trifluorobut-3-yl-2-ol represented by the formula (2) as a key intermediate of an AIDS therapeutic agent Efavirenz using an enantioselective trifluoromethylation reaction.SOLUTION: There is provided an enantioselective manufacturing method of a trifluoromethyl alcohol compound represented by the formula (2) by a high enantioselective trifluoromethylation reaction to alkynyl ketone by using a cinchona alkaloid phase transfer catalyst exemplified by the formula (4) and (trifluoromethyl)trimethylsilane.SELECTED DRAWING: None

Inventors:

OKUSU SATOSHI
TOKUNAGA ETSUKO
SHIBATA TETSUO

Application Number:

JP2015007675A

Publication Date:

July 25, 2016

Filing Date:

January 19, 2015

Export Citation:

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Assignee:

NAGOYA INST TECHNOLOGY

International Classes:

C07B53/00; B01J31/02; C07C201/12; C07C205/26

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