METHOD FOR SAFELY PREPARING PIMAVANSERIN AND TARTRATE SALT THEREOF USING TRIPHOSGENE - LIVZON NEW NORTH RIVER PHARMACEUTICAL CO LTD

Title:

METHOD FOR SAFELY PREPARING PIMAVANSERIN AND TARTRATE SALT THEREOF USING TRIPHOSGENE

Document Type and Number:

WIPO Patent Application WO/2020/020064

Kind Code:

A1

Abstract:

Disclosed in the present invention is a method for safely preparing pimavanserin and a tartrate salt thereof using triphosgene. The synthesis routes comprise (1), (2), (3), (4) and (5). The raw materials used in the method of the present invention are safe, and have low cost, effectively reducing the production cost. The reaction conditions of the method of the present invention are mild, the use of phosgene, having high toxicity and being difficult to operate, can be avoided, and the method is easy to implement industrially.

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Inventors:

JIANG QIAO (CN)
LI BINGBING (CN)
PENG MURONG (CN)
XIE WEIJIAN (CN)

Application Number:

PCT/CN2019/096705

Publication Date:

January 30, 2020

Filing Date:

July 19, 2019

Export Citation:

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Assignee:

LIVZON NEW NORTH RIVER PHARMACEUTICAL CO LTD (CN)

International Classes:

C07C51/41; C07D211/58; C07C59/255; C07C213/02; C07C217/58

Domestic Patent References:

WO2016141003A1

2016-09-09

Foreign References:

CN108947891A	2018-12-07
CN108794351A	2018-11-13
CN106588753A	2017-04-26
CN101778821A	2010-07-14
CN105820110A	2016-08-03
CN106946764A	2017-07-14
CN105111135A	2015-12-02
CN105418460A	2016-03-23
CN201610302251A	2016-05-09
US7790899B2	2010-09-07
US7601740B2	2009-10-13

Other References: