The synthetic method of varenicline

A technique for varenicline and compounds, applied in the field of preparation of intermediate compounds, capable of solving problems such as expensive reagents and/or catalysts, high cost, safety issues, operating conditions, etc.
CN113185513BActive Publication Date: 2022-05-31唐山臻越科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
唐山臻越科技有限公司
Publication Date
2022-05-31

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Abstract

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

Synthetic method of varenicline technical field

[0001] The present invention relates to a process for preparing varenicline or a pharmaceutically acceptable salt thereof. The invention also relates to the Useful intermediate compounds in the process and preparation of such intermediate compounds. Background technique Varenicline (Varenicline), chemically called 7,8,9,10-tetrahydro-6,10-methylene-6H-pyrazino [2,3‑h][3]benzazepine is represented by formula (1).

[0003] Varenicline and its pharmaceutical salts, such as varenicline tartrate, are available as CHANTIX by Pfizer TM product name pin It is sold as a selective partial agonist of nicotinic receptors for certain subtypes, which can be used for smoking cessation.

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

[0006]

[0007] Formu...

Claims

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