Title:
SUVOREXANT INTERMEDIATE AND PREPARATION METHOD THEREOF
Document Type and Number:
WIPO Patent Application WO/2017/133620
Kind Code:
A1
Abstract:
The present invention relates to a synthesis process of suvorexant, and a preparation method of novel compounds represented by formulas II, III, IV or V, or a salt or intermediate thereof for preparing the suvorexant. The preparation method uses a chiral initiator to synthesize chiral compounds represented by formulas II, III, IV or V, the compound obtained being used for synthesizing the suvorexant. The preparation method has the advantages of simple operation, low cost, mild reaction conditions, simple post-treatment, easy purification, high yield, high ee value, and ease of industrialization. In the reaction route shown, R represents a benzyl, allyl or 1-phenethyl group, or a benzyl group wherein the second to sixth carbon atoms are arbitrarily substituted, such as a 4-methoxybenzyl, 4-nitrobenzyl, 2-methylbenzyl, 4-chlorobenzyl or 3-fluorobenzyl group.
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Inventors:
LIN JIANPING (CN)
GUO XIAOWEN (CN)
GAO XIAOFEI (CN)
HUANG CHAO (CN)
GUO YUANBING (CN)
TAO ANPING (CN)
HUANG LUNING (CN)
GU HONG (CN)
GUO XIAOWEN (CN)
GAO XIAOFEI (CN)
HUANG CHAO (CN)
GUO YUANBING (CN)
TAO ANPING (CN)
HUANG LUNING (CN)
GU HONG (CN)
Application Number:
PCT/CN2017/072624
Publication Date:
August 10, 2017
Filing Date:
January 25, 2017
Export Citation:
Assignee:
ZHEJIANG HUAHAI PHARM CO LTD (CN)
SHANGHAI AOBO PHARMTECH INC LTD (CN)
SHANGHAI AOBO PHARMTECH INC LTD (CN)
International Classes:
C07D413/04; C07C269/06; C07C271/22; C07D243/08; C07D413/14
Domestic Patent References:
| WO2008069997A1 | 2008-06-12 | |||
| WO2012148553A1 | 2012-11-01 | |||
| WO2013169610A1 | 2013-11-14 | |||
| WO2016020406A1 | 2016-02-11 | |||
| WO2016020405A1 | 2016-02-11 | |||
| WO2016020404A1 | 2016-02-11 |
Other References:
YIN, CHEN ET AL.: "Facile Synthesis of Suvorexant, an Orexin Receptor Antagonist, via a Chiral Diazepane Intermediate", CHINESE CHEMICAL LETTERS, 31 January 2015 (2015-01-31), pages 103 - 107, XP029132725, Retrieved from the Internet
STROTMAN, N. ET AL.: "Reaction Development and Mechanistic Study of a Ruthenium Catalyzed Intramolecular Asymmetric Reductive Amination en Route to the Dual Orexin Inhibitor Suvorexant ( MK -4305)", JACS, vol. 133, 2 May 2011 (2011-05-02), pages 8362 - 8371, XP055127239, Retrieved from the Internet
DATABASE REGISTRY [O] UKRORGSYNTEZ LTD.; 9 November 2011 (2011-11-09), "RN 1343179-52-1", retrieved from STN Database accession no. stn
See also references of EP 3412665A4
STROTMAN, N. ET AL.: "Reaction Development and Mechanistic Study of a Ruthenium Catalyzed Intramolecular Asymmetric Reductive Amination en Route to the Dual Orexin Inhibitor Suvorexant ( MK -4305)", JACS, vol. 133, 2 May 2011 (2011-05-02), pages 8362 - 8371, XP055127239, Retrieved from the Internet
DATABASE REGISTRY [O] UKRORGSYNTEZ LTD.; 9 November 2011 (2011-11-09), "RN 1343179-52-1", retrieved from STN Database accession no. stn
See also references of EP 3412665A4
Attorney, Agent or Firm:
PATENTSINO IP FIRM (CN)
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