Method for preparing Roxadustat intermediate

A technology for intermediates and compounds, which is applied in the preparation of imino compounds, organic chemistry, etc., can solve the problems of difficult quality purification of the final product API, cumbersome preparation process, and high preparation cost, and achieves easy availability of raw materials and high reaction yield. , the effect of fewer steps
CN106478504AActive Publication Date: 2017-03-08SHANGHAI XUNHE PHARMA TECH CO LTD
5 Cites 23 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI XUNHE PHARMA TECH CO LTD
Publication Date
2017-03-08

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention provides a preparation method of Roxadustat intermediate 4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinecarboxylate (IV), comprising the step of subjecting 2-(1-(3-phenoxyphenyl)ethylimide)dimalonate (III) as a starting material to condensation and cyclization. The preparation method of the Roxadustat intermediate IV has the advantages that material is easy to obtain, operating steps are few, the process is simple, the reaction yield is high, atom utilization rate is high, and the method is easy for industrial production. The reaction general formula is shown in the specification.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention relates to a preparation method of Roxadustat intermediate used for treating chronic anemia. Background technique

[0002] Roxadustat is an oral hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor originally developed by FibroGen in the United States and currently co-developed with AstraZeneca. The chemical name is N-[(4-hydroxy-1-methyl-7 -Phenoxy-3-isoquinolinyl)carbonyl]glycine, this product can be used for the treatment of chronic anemia, and is currently in Phase 3 clinical research stage in the US FDA.

[0003] The method that prior art is used for preparing Roxadustat mainly contains:

[0004] 1) The compound patent synthesis route of the original FibroGen company (CN102977015B, application date: 20040604), as shown in the following scheme:

[0005]

[0006] 2) Zhejiang Beida announced the following synthetic method (CN104024227B, application date: 20120723) to improve the patented method of the original research compo...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More