Preparation process of isosorbide mononitrate

A technology of nitric acid and sorbitol, which is applied in the fields of cardiovascular system diseases, organic chemistry, drug combination, etc., and can solve problems such as complex, difficult to control reactions, and high cost

Inactive Publication Date: 2005-05-25
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The process operation of the above route is relatively complicated, the reaction is difficult to control, the yield is low, and the cost is high, and some routes use xylene, benzene and other toxic solvents, which have great pollution to the environment

Method used

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  • Preparation process of isosorbide mononitrate
  • Preparation process of isosorbide mononitrate
  • Preparation process of isosorbide mononitrate

Examples

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example 1

[0018] Synthesis of intermediate 1, 4:3,6-dianhydro-D-sorbitol: 310 grams of 70% sorbitol were slowly added to 9.5 milliliters of p-toluenesulfonic acid at 40 ° C under stirring, and then the Slowly raise the temperature to evaporate the water under a certain vacuum, and the water will be basically evaporated when it rises to about 117°C. The vacuum is 0.096Mpa, and the sorbitan is collected below 220°C, with a yield of 91%.

[0019]

example 2

[0021] Preparation of compound (4): Add 100 grams of sorbitan to 180 milliliters of acetic acid, stir and heat up to dissolve, then add 5 grams of N,N-dimethylaminopyridine, stir at 30°C for 10 minutes, then add acetic anhydride dropwise at 45°C, and the addition is complete After that, continue to keep warm at 45°C for 30 minutes, drop to 20°C, stir and keep warm for 2 hours, then filter to obtain solid compound (4). Yield 95%.

[0022]

example 3

[0024] Preparation of nitrating agent: After stirring and mixing 38ml of acetic anhydride and 32ml of acetic acid, slowly add 14ml of nitric acid dropwise, keep the temperature at 15°C-20°C during the dropwise addition, and keep warm at 15°C for later use.

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Abstract

A process for preparing the isosorbide mononitrate from sorbitol includes dewatering sorbitol by p-methylphenyl sulfonic acid to obtain anhydrosorbitol, protecting by acetic oxide under existance of N,N-dimethylaminopyridine, nitrating by nitric acid / acetic oxide / acetic acid system, and removing protection by potassium carbonate-methanol system. It can be used to treat angina pectoris.

Description

technical field [0001] The invention relates to a preparation method of the compound isosorbide mononitrate (1,4:3,6-dianhydro-D-sorbitol-5-nitrate), which belongs to the fields of chemical industry and chemical medicine. Background technique [0002] Isosorbide Mononitrate is the general name of 1,4:3,6-dianhydro-D-sorbitol-5-nitrate, and its structural formula is: [0003] [0004] It is a long-acting nitrate antianginal drug, which was discovered in the metabolites of isosorbide dinitrate in the body in the 1960s. In the 1980s, it was first introduced to the market by Bochringer Cnbh in Germany, and then it has been listed in more than ten countries in Europe and America, and has been widely used in clinical practice. my country imported the drug in 1988, and it was widely welcomed by patients. Its synthetic route mainly contains: [0005] [0006] [0007] Other synthetic routes also adopt (C 6 h 5 ) 3 CCl, CH 3 SO 2 After protecting the sorbitan with Cl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P9/10C07D493/04
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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