Varenicline synthesis method

A technology for varenicline and compounds, applied in the field of preparation of intermediate compounds, can solve problems such as inconvenience, safety problems, operating conditions, expensive reagents and/or catalysts, etc.
CN113185513AActive Publication Date: 2021-07-30唐山臻越科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
唐山臻越科技有限公司
Publication Date
2021-07-30

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Abstract

The present invention relates to a process for the preparation of varenicline or a pharmaceutically acceptable salt thereof. The invention also relates to an intermediate compound useful in the process and the preparation of such intermediate compound.
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Description

technical field

[0001] The invention relates to a process for preparing varenicline or a pharmaceutically acceptable salt thereof. The invention also relates to intermediate compounds useful in this process and the preparation of such intermediate compounds. Background technique

[0002] Varenicline, chemically known as 7,8,9,10-tetrahydro-6,10-methylene-6H-pyrazino[2,3-h][3]benzazepine , represented by formula (1).

[0003]

[0004] Varenicline and its pharmaceutical salts, such as varenicline tartrate, marketed by Pfizer as CHANTIX TM Marketed as a selective partial agonist of nicotinic receptors for certain subtypes, it is useful for smoking cessation.

[0005] The synthesis of varenicline and its pharmaceutical salts are described in US6410550B1, US6890927B2, US2008 / 0275051A1, US8314235B2 and WO2018163190A1. Most of the reported methods involve the following process:

[0006]

[0007] Formula (2) is nitrated to obtain formula (3), followed by reduction and cyc...

Claims

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