Title:
METHOD FOR PREPARING LEMBOREXANT AND METHOD FOR PREPARING LEMBOREXANT INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2023/178693
Kind Code:
A1
Abstract:
Provided in the present invention is a method for preparing lemborexant, which method comprises the following steps: subjecting compound II and compound III as raw materials to a reaction in a second reaction solvent to obtain lemborexant. Further provided in the present invention is a method for preparing compound II. The prepared compound II of the present invention is an active ester intermediate of Oxyma, has a high reaction activity, and is a safe and non-explosive auxiliary nucleophile. According to the present invention, the use of traditional activators such as HOBt and HOAT is avoided, thereby eliminating potential safety hazards; and by using the method of the present invention to prepare lemborexant, the reaction is safe and efficient, and the racemization rate of the obtained product is low.
Inventors:
SHEN JIJUN (CN)
MU YONGLE (CN)
JIAN ZHENGJUN (CN)
HE XIANLIANG (CN)
HUANG LUNING (CN)
TAO ANPING (CN)
GU HONG (CN)
MU YONGLE (CN)
JIAN ZHENGJUN (CN)
HE XIANLIANG (CN)
HUANG LUNING (CN)
TAO ANPING (CN)
GU HONG (CN)
Application Number:
PCT/CN2022/083178
Publication Date:
September 28, 2023
Filing Date:
March 25, 2022
Export Citation:
Assignee:
ZHEJIANG HUAHAI PHARM CO LTD (CN)
SHANGHAI SYNCORES TECH INC LTD (CN)
SHANGHAI SYNCORES TECH INC LTD (CN)
International Classes:
C07D239/34; C07C29/147; C07C67/14; C07C69/16; C07D239/28; C07D401/12
Foreign References:
| CN103153963A | 2013-06-12 | |||
| CN104114524A | 2014-10-22 | |||
| CN113727962A | 2021-11-30 | |||
| CN112672992A | 2021-04-16 | |||
| US20120165339A1 | 2012-06-28 |
Other References:
DI MAN, GUO LIYUAN, KONG LU, HE ZIRU, HUANG SHENGTANG, WU SHI: "Oxyma and Its Derived Novel Coupling Reagents", JOURNAL OF HUBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY (MEDICAL SCIENCES), vol. 33, no. 3, 30 June 2019 (2019-06-30), pages 267 - 272, XP009548986, ISSN: 2095-4646, DOI: 10.16751/j.cnki.2095-4646.2019.03.0267
SUBIROS-FUNOSAS, R. ET AL.: "Oxyma: An Efficient Additive for Peptide Synthesis to Replace the Benzotriazole-Based HOBt and HOAt with a Lower Risk of Explosion", CHEMISTRY-A EUROPEAN JOURNAL, vol. 15, no. 37, 14 September 2009 (2009-09-14), pages 9394 - 9403, XP055025877, ISSN: 1521-3765, DOI: 10.1002/chem.200900614
SUBIROS-FUNOSAS, R. ET AL.: "Oxyma: An Efficient Additive for Peptide Synthesis to Replace the Benzotriazole-Based HOBt and HOAt with a Lower Risk of Explosion", CHEMISTRY-A EUROPEAN JOURNAL, vol. 15, no. 37, 14 September 2009 (2009-09-14), pages 9394 - 9403, XP055025877, ISSN: 1521-3765, DOI: 10.1002/chem.200900614
Attorney, Agent or Firm:
PATENTSINO IP FIRM (CN)
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