Preparation method for intermediate of Roxadustat

A technology for intermediates and compounds, which is applied in the preparation of acyl halides, carboxylic acid halides, sulfonamides, etc., can solve the problems of difficult quality purification of final product raw materials, cumbersome preparation process, and high preparation costs, and achieve operational Convenience, high reaction yield, easy access to raw materials
CN106478503AInactive Publication Date: 2017-03-08SHANGHAI XUNHE PHARMA TECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHANGHAI XUNHE PHARMA TECH CO LTD
Publication Date
2017-03-08
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a preparation method for an intermediate VI of Roxadustat. The preparation method comprises the following steps: reacting 3-methyl-5-bromoisobenzofuran-1(3H)-one (I), which serves as a starting raw material, with phenol so as to prepare an intermediate II, then, subjecting the II to a ring-opening substitution reaction so as to prepare a compound III, and subjecting the compound III to a substitution reaction so as to prepare a key intermediate V; and subjecting the V to alkali condensation, deprotection and aromatization, thereby preparing the target intermediate VI. The preparation method for the intermediate VI of the Roxadustat, provided by the invention, has the advantages that the raw materials are readily available, the process is simple, the operation is convenient, the reaction yield is high, the atom utilization ratio is high, and the industrial production is facilitated. The reaction general formula is represented by the formulae shown in the description.
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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

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