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Varenicline salt and preparing method thereof

A varenicline and tartrate technology, applied in the field of anti-nicotine addiction drug varenicline salt and its preparation, can solve the problems of performance such as solubility and thermal stability without detailed evaluation and the like

Active Publication Date: 2014-07-02
SHANGHAI SYNCORES TECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although a large number of varenicline salts are disclosed in many patents, no detailed evaluation has been given on the properties of various salts such as solubility and thermal stability

Method used

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  • Varenicline salt and preparing method thereof
  • Varenicline salt and preparing method thereof
  • Varenicline salt and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Dissolve 3g of varenicline in 25ml of ethanol, dissolve 1.02g of tartaric acid in 10ml of ethanol, slowly add the ethanol solution of L-tartaric acid into the ethanol solution of varenicline under stirring, after the addition is complete, heat up to 70°C, Add 4.5ml of water until it is just clear, maintain this temperature for 10 minutes, let it stand still, a large amount of off-white solid precipitates, filter it with suction, and dry it in vacuum to obtain 2.8g of off-white solid, with a yield of 68.9%.

Embodiment 2

[0040] Dissolve 3g of varenicline in 20ml of acetone, dissolve 1.02g of tartaric acid in 5ml of water, slowly add the aqueous solution of L-tartaric acid into the acetone solution of varenicline under stirring, after the addition is complete, heat up to 55°C, add 2.6 ml of water until it is just clear, maintain this temperature for 10 minutes, let it stand still, a large amount of off-white solid precipitates, filter it with suction, and dry it in vacuum to obtain 3.3 g of off-white solid, with a yield of 81.2%.

Embodiment 3

[0042] Dissolve 3g of varenicline in 20ml of methanol, dissolve 1.02g of tartaric acid in 5ml of methanol, slowly add the methanol solution of L-tartaric acid into the methanol solution of varenicline under stirring, after the addition is complete, heat up to 65°C, Add 1.5ml of water until it is just clear, maintain this temperature for 10 minutes, let it stand still, a large amount of off-white solid precipitates, filter it with suction, and dry it in vacuum to obtain 2.5g of off-white solid, with a yield of 61.6%.

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Abstract

The invention relates to varenicline hemitartrate and a preparing method thereof. The salt has a structure shown as the formula II. The varenicline hemitartrate is good in stability, low in moisture adsorption and high in safety. The preparing method is simple in operation and good in reproducibility.

Description

technical field [0001] The invention relates to an anti-nicotine addiction medicine varenicline salt and a preparation method thereof. Background technique [0002] The compound of the structure shown in formula I is the parent structure of the anti-nicotine addiction drug varenicline, and its chemical name is: 7,8,9,10-tetrahydro-6,10-methylene-6H-pyrazino[ 2,3-h][3]Benzazepine, developed by Pfizer. In May and September 2006, varenicline tartrate was approved for marketing by the US FDA and the European EMEA respectively. [0003] [0004] In general, the use of pharmaceutically acceptable salts of pharmaceutical compounds is also true for anti-nicotine addiction drugs such as compounds of formula I, which makes the preparation of pharmaceutically acceptable salts of such compounds particularly important. In this regard, predecessors have also done some work in this area. [0005] Patent CN100370987 discloses three crystal forms A, B and C of the L-tartrate salt of th...

Claims

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Application Information

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IPC IPC(8): C07D471/18C07C59/255C07C51/41
CPCC07D471/08
Inventor 王举波司永星方干武文举张席妮
Owner SHANGHAI SYNCORES TECH INC
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