Improvement of nortropine synthesizing process

A technology of nortropine alcohol and tropine alcohol, which is applied in organic chemistry and other fields, and can solve problems such as side reactions and affecting product purity

Active Publication Date: 2010-06-30
YANGTZE RIVER PHARM GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem that this preparation method exists is that chloroform can react with alkali to generate active intermediate dichlorocarbene under the condition that strong alkali exists, and side reaction occurs; In ...

Method used

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Examples

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Embodiment Construction

[0014] Mix 168g (1.5mol) of ethyl chloroformate and 500ml of chloroform into a 2L there-necked flask, and heat to reflux; dissolve 50g (0.35mol) of tropinol in 200ml of chloroform and then slowly add it to the above-mentioned reflux solution, and react White mist is generated during the process. After the dropwise addition, continue to reflux for 2 hours, stop heating and stirring. Concentrate to obtain a colorless oil, then add 10% KOH aqueous solution, and heat to reflux for about 12 hours. Cool to room temperature, extract with 500ml chloroform, extract 4 times, and wash the chloroform layer with saturated brine once more. After the chloroform layer was concentrated, 38.5 g of a reddish-brown oily substance was obtained, and the yield was 85%.

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Abstract

The invention discloses an improvement method of a nortropine synthesizing process. In the method, tropine and ethyl chloroformate are adopted as raw materials to synthesize nortropine. By adjusting the experimental operating steps, the method achieves the effects of moderate reaction condition, safe, simple as well as convenient operation, good product quality, and low cost.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and in particular relates to a method for improving the synthesis process of nortropine alcohol. Background technique [0002] Overactive bladder (OAB) is a common and distressing problem, a common disease that affects the normal life of people of different ages, both men and women, especially women and the elderly. At present, the incidence rate of this disease is very high. According to the survey in Beijing area of ​​my country, the incidence rate of urinary incontinence in men over 50 years old is 16.4%, and the total incidence rate of mixed urinary incontinence and urge urinary incontinence in women over 18 years old is as high as 40.4%. [0003] Trospium chloride is a quaternary ammonium compound and belongs to the anticholinergic class of muscarinic receptor blockers. These drugs relax bladder smooth muscle, thereby reducing bladder contractions, and can be used as long-term treatm...

Claims

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Application Information

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IPC IPC(8): C07D451/10
Inventor 赵文镜冯建鹏高力虎张虎跃朱年青霍浩刚
Owner YANGTZE RIVER PHARM GRP CO LTD
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