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A kind of preparation method of perindopril arginine

A technology of perindopril arginine and arginine, which is applied in the field of preparation of perindopril arginine, can solve the problems of difficult industrial operation, unsatisfactory properties of perindopril arginine treatment, and stable perindopril Poor performance, difficult preparation and purification, etc., to achieve the effect of improving product yield

Active Publication Date: 2022-06-14
NANJING GRITPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the above public documents, it is necessary to use perindopril as a raw material to react with arginine, but perindopril has poor stability and is not easy to prepare and purify, and perindopril arginine has unsatisfactory post-treatment properties according to the above documents and is not easy to be industrialized. Therefore, it is necessary to develop a method for preparing perindopril arginine that is more suitable for technological production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment ( 1

[0023] Add 70.0g of tert-butylamine perindopril, 26.2g (0.95eq) of L-arginine, and 210g of purified water to a 2L reaction flask, stir until the reaction solution is clear, add 770g of dimethyl sulfoxide, and heat to 40-50°C React, and keep the negative pressure <-0.07Mpa to react for one hour, add 273g of ethyl acetate after the reaction, cool down to 5-25°C for crystallization for 4 hours, suction filter the obtained solid, rinse the solid with ethyl acetate and place it in vacuum drying , the obtained solid was washed twice with ethyl acetate and filtered with suction, and finally dried in vacuo for 4h. The yield is 82.3%, and the purity is 99.96%.

Embodiment ( 2

[0025] Add 100 g of perindopril isopropylamine, 39.4 g (1 eq) of L-arginine to 220 g of purified water in a 5L reaction flask, stir until the reaction solution is clear, add 660 g of dimethyl sulfoxide, heat up to 40-50 ° C and keep Negative pressure <-0.07Mpa and react for one hour. After the reaction, methyl tert-butyl ether was added, and the temperature was lowered to 0-10 °C for crystallization for 6 hours. After drying, the obtained solid was washed twice with methyl tert-butyl ether and filtered with suction. Finally, the yield was 87.5% and the purity was 99.94% after vacuum drying for 6 hours.

Embodiment ( 3

[0027] Add 50 g of perindopril diethylamine and 17.8 g (0.9 eq) of L-arginine to a 2L reaction flask, stir until the reaction solution is clear, add 350 g of dimethyl sulfoxide, add isopropyl acetate, and cool to 0 Crystallize at -10°C for 12 hours, filter the obtained solid, rinse the solid with isopropyl acetate and place it in vacuum to dry, and then stir the obtained solid with isopropyl acetate for 2 times and filter it with suction. Finally, the yield is vacuum dried for 6 hours. 83.3%, purity 99.92%.

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Abstract

The invention belongs to the field of drug synthesis and relates to a preparation method of perindopril arginine. The preparation method of perindopril arginine of the present invention is that an organic amine salt of perindopril is reacted with L-arginine to obtain perindopril arginine. The perindopril arginine prepared by the invention is in the form of white powder, the purity of which can reach more than 99.9%, and the yield is more than 80%.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a preparation method of arginine perindopril. Background technique [0002] Arginine perindopril is a drug for the treatment of mild to moderate essential hypertension launched by French company Servier. Compared with tert-butylamine perindopril, the compound is more stable and the shelf life can be extended to more than 2 years. And arginine perindopril can be combined with amlodipine besylate to form a compound preparation for the treatment of adult patients with hypertension that cannot be adequately controlled by a single drug. [0003] CN101389603 relates to a preparation method of α crystal form, which uses DMSO, water and methylcyclohexane as solvents to prepare hydrate; CN101389604 relates to a preparation method of β crystal form, which passes arginine perindopril α crystal form through Toluene or acetonitrile is refluxed at high temperature to prepare the anhydrous β crys...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C277/08C07C279/14C07K5/062
CPCC07C277/08C07K5/06026C07C279/14
Inventor 李先喆邓书兰耿聪聪魏伟业赵卿霍立茹李战
Owner NANJING GRITPHARMA CO LTD
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