METHODS OF PREPARING BREXPIPRAZOLE, KEY INTERMEDIATES THEREOF AND SALTS THEREOF

Title:

METHODS OF PREPARING BREXPIPRAZOLE, KEY INTERMEDIATES THEREOF AND SALTS THEREOF

Document Type and Number:

WIPO Patent Application WO/2015/054976

Kind Code:

A1

Abstract:

The present invention relates to methods of preparing brexpiprazole, analogs thereof, key intermediates and salts thereof. Specifically, the present invention relates to new methods of preparing brexpiprazole, analogs thereof, key intermediates and salts thereof, and to the key intermediates and salts thereof used in the methods. The methods involve mild reaction conditions, stable intermediates, easy operations, and widely available reagents, thereby allowing for reduced synthesis costs, a shortened production cycle, high yield, and high product quality. The methods are suited for use in large-scale production.

Inventors:

LIU ZHENG (CN)
WU CHUNHUI (CN)
LIU YONGJIAN (CN)
ZHANG RONGXIA (CN)
HE YANG (CN)
TIAN GUANGHUI (CN)
SHEN JINGSHAN (CN)

Application Number:

PCT/CN2014/000921

Publication Date:

April 23, 2015

Filing Date:

October 20, 2014

Export Citation:

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Assignee:

SUZHOU VIGONVITA LIFE SCIENCES CO LTD (CN)
TOPHARMAN SHANGHAI CO LTD (CN)
SHANGHAI INST MATERIA MEDICA (CN)

International Classes:

C07D409/12; C07D333/70

Domestic Patent References:

WO2009128537A1	2009-10-22
WO2006112464A1	2006-10-26
WO2013015456A1	2013-01-31
WO2006112464A1	2006-10-26
WO2013015456A1	2013-01-31

Foreign References:

US5436246A	1995-07-25
US5436246A	1995-07-25

Other References: