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Title:
METHOD FOR SYNTHESIS OF ROXADUSTAT AND INTERMEDIATE COMPOUNDS THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/114811
Kind Code:
A1
Abstract:
The present application provides a method for synthesis of Roxadustat. A compound as represented by formula (VIII) is used as a raw material, and is reacted with phenol, a vinyl-containing ether, an acid, hydroxylamine, and then the product is reacted with glycine. In addition, the present application also provides intermediate compounds as represented by formula (IX), formula (XI), formula (XII), formula (IV), and formula (V) for synthesis of Roxadustat. Here, details of the substituents involved in formula (VIII), formula (IX), formula (XI), and formula (XII) are stated in the description.

Inventors:
XU, Yongxiang (Jiangsu Life Sciences & Technology Innovation Park Building 28, No.9 Weidi Road Xianlin University City, Nanjing Jiangsu 3, 210033, CN)
Application Number:
CN2018/121082
Publication Date:
June 20, 2019
Filing Date:
December 14, 2018
Export Citation:
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Assignee:
NANJING CAVENDISH BIO-ENGINEERING TECHNOLOGY CO., LTD. (Jiangsu Life Sciences & Technology Innovation Park Building 28, No.9 Weidi Road Xianlin University City, Nanjing Jiangsu 3, 210033, CN)
XU, Yongxiang (Jiangsu Life Sciences & Technology Innovation Park Building 28, No.9 Weidi Road Xianlin University City, Nanjing Jiangsu 3, 210033, CN)
International Classes:
C07D217/26; C07C65/40; C07C69/92; C07D265/02
Domestic Patent References:
WO2018039310A12018-03-01
WO2018005591A12018-01-04
WO2017111787A12017-06-29
Foreign References:
CN108794397A2018-11-13
CN104024227A2014-09-03
CN103435546A2013-12-11
CN104892509A2015-09-09
CN106083720A2016-11-09
Other References:
ABDOU, WAFAA MAHMOUD ET AL.: "Study of Insertion Reactions with Phosphorus Ylides on Reactions between 4-(4-Methylphenyl)-2,3- benzoxazin-l-one and Alkylidene Phosphoranes", EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, vol. 2002, 16 April 2002 (2002-04-16), pages 1696 - 1701, XP055617384, ISSN: 1434-193X
KAMEL, AZZA A.: "An Efficient Route to Phosphono-Substituted-Indoles and Qui- nolines from the Condensation of 2,3-and 2,4-Benzoxazin-1-0nes with alpha-Pho- sphonyl Carbanions", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS, vol. 182, no. 4, 24 February 2007 (2007-02-24), pages 765 - 777, XP055617385, ISSN: 1042-6507
Attorney, Agent or Firm:
AFD CHINA INTELLECTUAL PROPERTY LAW OFFICE (Suite B 1601A, 8 Xue Qing Rd. Haidian, Beijing 2, 100192, CN)
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