Synthesis method of baloxavir marboxil intermediate

A synthesis method and compound technology, applied in organic chemistry and other directions, can solve the problems of few synthesis routes, difficult production control, purchase and use restrictions, etc., and achieve the effect of facilitating industrial production, avoiding potential dangers, and solving toxicity problems.
CN110143941AActive Publication Date: 2019-08-20BEIJING SIHUAN PHARMA +2
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
BEIJING SIHUAN PHARMA
Publication Date
2019-08-20

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Abstract

The invention provides a synthesis method of a baloxavir marboxil intermediate. The invention provides a synthesis method of a compound (III), which is prepared through three steps. The yield is improved, and the production is easy to control. At the same time, a synthesis method of a compound (IV) is provided. According to the synthesis method, the compound (III) and disulfide diphenyl carry outone-pot self-catalytic circulation reactions to generate the compound (IV). The invention provides a method for preparing a baloxavir marboxil intermediate (VIII) through the reactions mentioned above. Through the one-pot self-catalytic circulation reactions, thiophenol, which is strongly toxic and is strictly controlled, is not used, a safe baloxavir marboxil synthesis method is provided, and thesynthesis method is suitable for industrial production.
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Description

technical field

[0001] The invention relates to a synthesis method of a pharmaceutical intermediate, in particular to a newly discovered "one-pot self-catalysis cycle" reaction and a method for preparing a barosavir-marbolate intermediate. Background technique

[0002] Influenza is an acute respiratory infectious disease caused by influenza virus. The World Health Organization estimates that there are approximately 3 million to 5 million influenza cases each year, resulting in approximately 250,000 to 500,000 deaths. Barosavir Marbolate is a new anti-influenza drug developed by Shionogi Company. It was approved for marketing in Japan on February 23, 2018, and is used for the treatment of influenza A and B in adults and children. Barosavir marbolate is the first anti-influenza drug with a new mechanism of action in the past 20 years. It inhibits the transcription and replication of influenza virus by inhibiting the cap-dependent endonuclease of influenza virus. The mechanism...

Claims

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