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Novel method for preparing sarpogrelate hydrochloride

A technology of sarcogrelate hydrochloride and sarcogrelate hydrochloride, which is applied in the field of preparation of sarcogrelate hydrochloride, can solve problems such as inconvenient operation, difficult crystallization, and unresolved synthesis problems, and achieve the effect of easy operation

Pending Publication Date: 2020-10-23
无锡道科森医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method uses an additional catalyst and also involves a high pressure reaction, so it is inconvenient to operate
[0005] CN103242179 is more focused on solving the crystallization difficulties of the final product, but the synthesis problem has not been solved

Method used

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  • Novel method for preparing sarpogrelate hydrochloride
  • Novel method for preparing sarpogrelate hydrochloride
  • Novel method for preparing sarpogrelate hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Step 1 (solvent-free condensation)

[0035]

[0036] Epichlorohydrin (303.9 g) was added to a mixture of 2,3-MPP (150 g) and NaOH (31.5 g) in RB at room temperature and heated at 48 to 52 °C for 3 hours. Another batch of NaOH (5.3 g) was added and heating was continued for 1 h. The reaction was cooled to room temperature and toluene (300ml) was added. The resulting suspension was passed through a bed of water and the filtrate was washed with brine solution (300ml). The volatiles were evaporated in vacuo to give 186 g of a brown oily material.

[0037] analyze:

[0038] MS:284.3(M+H) +

[0039] Step two (ethylene oxide opening)

[0040]

[0041] To a solution of the step 1 intermediate (186 g) in 2-methyl THF (600 ml) was added 40% aqueous dimethylamine (588.7 g) at 5°C. The temperature of the addition was raised to room temperature and stirred for 3h. The reaction mixture was washed with brine solution (300ml). The volatiles were evaporated in vacuo and t...

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Abstract

The invention aims to disclose sarpogrelate hydrochloride prepared by a convenient and environment-friendly method, relates to a solvent, in particular to a solvent which is prepared by free condensation of 2-[2-(3-methoxyphenyl) ethyl] phenol and epoxy chloropropane (2-[2-(3-metoxypherol) ethyl] pherol withepoxychloropropane). Under atmospheric pressure, dimethylamine is used for ring opening ofethylene oxide of the obtained intermediate, and then the intermediate reacts with succinic anhydride to obtain sarpogrelate. The obtained free alkali is treated by using isopropanol IPA.HCl to obtainthe sarpogrelate hydrochloride. Crystals of hydrochloride are formed in acetone, and a pure product is obtained. According to the preparation method, solvent-free reaction is adopted in the first step, atmospheric pressure reaction is adopted in the second step, and thus the preparation method is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a convenient and environment-friendly new method for preparing sagrelate hydrochloride. Background technique [0002] Sarpogrelate hydrochloride (Sarpogrelate) was developed and sold by Mitsubishi Tanabe Pharmaceuticals in Japan in 1993. It is a platelet aggregation inhibitor with a new mechanism of action, which can selectively antagonize the serotonin receptor (5-HT2). Sagrelate can inhibit platelet aggregation, inhibit vasoconstriction, have antithrombotic effect and improve microcirculation. Its indication is to improve all ischemic symptoms caused by chronic arterial occlusive diseases, such as ulcers, pain and peristaltic cold. It also has potential for use in the treatment of diabetes, thromboangiitis obliterans (Berger's disease), Raynaud's syndrome, coronary artery disease, angina, and atherosclerosis. [0003] The initial synthesis of sargrel hydrochloride is discl...

Claims

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Application Information

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IPC IPC(8): C07C219/06C07C213/00
CPCC07C213/02C07C213/00C07D301/28C07C217/34C07C219/06
Inventor 克里斯蒂安·山多夫
Owner 无锡道科森医药有限公司
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