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Synthesis method for sarpogrelate hydrochloride

A technology for sarpogrelate hydrochloride and a synthesis method, which is applied in chemical instruments and methods, preparation of organic compounds, preparation of aminohydroxy compounds, etc., can solve the problems of cumbersome process, long route, difficult control and the like, and achieves simple synthesis route and purity Good, prevent catalyst poisoning effect

Inactive Publication Date: 2019-05-31
ANHUI HERYI CHEM
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In order to reduce costs, it is necessary to control the residual phosphorus in olefin intermediates by recycling palladium-carbon catalysts, which is cumbersome and increases costs.
From the perspective of the whole technology, the route is long, the process is complicated and difficult to control, and the cost is high

Method used

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  • Synthesis method for sarpogrelate hydrochloride
  • Synthesis method for sarpogrelate hydrochloride
  • Synthesis method for sarpogrelate hydrochloride

Examples

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Embodiment 1

[0017] Synthesis of Intermediate 8:

[0018] Under the protection of nitrogen, put 300g of intermediate 6 and 300g of intermediate 7 into a 1000mL glass reaction bottle, raise the temperature to 120±2°C, keep stirring for 5h, and the reaction ends. Slowly pour the reaction solution into 2000 mL of ice water, stir to precipitate an off-white solid, filter with suction, wash with water, and dry. Four times the amount of methanol was crystallized to obtain 371 g of off-white intermediate 8 with a yield of 85% and a purity of 98.6%.

[0019] Synthesis of intermediate 5:

[0020] Dissolve 371g of intermediate 8 in 1484g of methanol, replace the air with nitrogen, put in 11g of 5% palladium carbon, replace the nitrogen in the reaction bottle with hydrogen, and continue to pass hydrogen at 55±2°C, and maintain the hydrogen pressure in the reaction bottle at 2atm, and maintain until no hydrogen is absorbed. After the reaction was completed, the hydrogen gas was vented, the palladiu...

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Abstract

The invention discloses a synthesis method for sarpogrelate hydrochloride, and relates to the technical field of medicine organic synthesis. Methoxyl diethyl phosphite 6 and 2-(3-dimethylamino-2-hydroxy)propoxybenzaldehyde 7 are adopted as raw materials, a condensing reaction is performed to generate a midbody 8, the midbody 8 generates a midbody 5 through a hydrogenation reduction reaction, the midbody 5 and butanedioic anhydride are subjected to an esterification reaction and a hydrochloric acid salt forming reaction to obtain sarpogrelate hydrochloride 1. The synthesis path is relatively simple, in the second step, hydrogenation reduction of double bonds is performed, hydroxyl protecting group benzyl is not needed, and therefore the requirement for catalysts is not strict, phosphorus residues of the midbody 8 do not need to be controlled strictly to prevent catalyst poisoning; meanwhile, the purity of the obtained midbody product 5 is good, and the high-purity target product can beobtained easily in the next step.

Description

Technical field: [0001] The invention relates to the technical field of organic synthesis of medicines, in particular to a synthesis method of sargrelate hydrochloride. Background technique: [0002] Sargrel hydrochloride, the chemical name is succinic acid mono[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl] Ethyl] ester hydrochloride is a 5-HT2 receptor antagonist and platelet aggregation antagonist developed by Tanabe Mitsubishi Pharmaceutical Co., Ltd. in Japan. It is clinically used for chronic thrombosis. [0003] At present, there are many routes for the synthesis of sargrelate hydrochloride, including the following synthetic routes: [0004] [0005] The route first utilizes o-benzyloxybenzyl diethyl phosphite 2 and m-methoxybenzaldehyde 3 to react to generate an alkene intermediate, and then uses palladium carbon catalyst for hydrogenation reduction and deprotection to obtain intermediate 4,4 Etherification with epichlorohydrin, ring-opening w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C213/06C07C219/06C07C213/08C07C217/32
CPCY02P20/55
Inventor 董来山
Owner ANHUI HERYI CHEM
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