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.

Active Publication Date: 2022-05-31
唐山臻越科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The above process has several disadvantages: inherently high cost due to long reaction sequences, expensive reagents and / or catalysts, safety concerns and inconvenient operating conditions

Method used

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  • The synthetic method of varenicline
  • The synthetic method of varenicline
  • The synthetic method of varenicline

Examples

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Embodiment Construction

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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.

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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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/08
CPCC07D471/08Y02P20/55
Inventor 周丽华
Owner 唐山臻越科技有限公司
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