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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.

Active Publication Date: 2021-07-30
唐山臻越科技有限公司
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  • Abstract
  • Description
  • Claims
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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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Examples

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Embodiment Construction

[0045] The following examples provide detailed experimental procedures and parameters suitable for the preparation of varenicline or a pharmaceutically acceptable salt thereof according to the present invention and are intended to be illustrative and not limiting.

[0046] Unless otherwise stated, all materials, solvents and reagents, including anhydrous solvents such as DMF and DCM, were obtained from commercial suppliers in the best grade and used without further purification. All reactions involving air- or moisture-sensitive compounds were performed under a nitrogen or argon atmosphere unless otherwise stated.

[0047] 1 H(400MHz) and 13 C NMR (100MHz) data using CDCl 3 or DMSO-D 6 Obtained as a solvent on Bruker AVANCE II 400MHz. Chemical shifts (δ) are in ppm and coupling constants (J) are in Hz. 1 H NMR spectrum is recorded with tetramethylsilane (δ=0.00ppm) as an internal reference; 13 C NMR spectrum with CDCl 3 (δ=77.00ppm) or DMSO-D 6 (δ = 39.5 ppm) was recor...

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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.

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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Application Information

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Patent Type & Authority Applications(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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