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New synthesis method of cinnarizine

A technology of cinnarizine and anhydrous piperazine, applied in the field of pharmaceutical preparation, can solve the problems of many by-products, difficult industrialized large-scale production, unfavorable purification and the like

Active Publication Date: 2013-08-21
珠海保税区丽珠合成制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The above two methods of synthesizing cinnarizine are relatively short in terms of steps, and the yield is also high, but there are many by-products, which are not conducive to purification, so it is difficult to be suitable for industrialized large-scale production

Method used

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  • New synthesis method of cinnarizine

Examples

Experimental program
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Effect test

Embodiment 1

[0044]Add 11mol / L zinc chloride solution (15ml, 0.165mol) and benzene (30ml, 0.155mol) into a 250ml three-necked flask, stir and raise the temperature until benzene refluxes, start to add 9.0g of benzyl chloride dropwise, and react for 4 hours after the dripping is completed. Set aside, separate the zinc chloride solution in the lower layer, add 180ml of water to the upper layer, stir for 5 minutes, let stand for 10 minutes, collect the organic phase, and rotary evaporate to dryness to obtain 26.0 g of diphenylmethane product, with a yield of 96% and a GC purity of 98%.

Embodiment 2

[0046] Add 11mol / L ferric chloride solution (15ml, 0.165mol) and benzene (30ml, 0.155mol) into a 250ml three-necked flask, stir and heat up to reflux of benzene, start to add 9.0g of benzyl chloride dropwise, and react for 4h after the dropwise completion. After standing still, separate the lower layer of zinc chloride solution, add 180ml of water to the upper layer, stir for 5 minutes, let stand for 10 minutes, collect the organic phase, and rotary evaporate to dryness to obtain 9.5g of diphenylmethane product, the yield is 35%, and the GC purity is 96%.

Embodiment 3

[0048] Add 11mol / L aluminum chloride solution (15ml, 0.165mol) and benzene (30ml, 0.155mol) into a 250ml three-necked flask, stir and raise the temperature to reflux of benzene, start to add 9.0g of benzyl chloride dropwise, and react for 4h after the dropwise completion. After standing still, separate the zinc chloride solution in the lower layer, add 180ml of water to the upper layer, stir for 5 minutes, let stand for 10 minutes, collect the organic phase, and rotary evaporate to dryness to obtain 20.6g of diphenylmethane product, with a yield of 76% and a GC purity of 96%.

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Abstract

The invention provides a new synthesis method of cinnarizine. The method consists of four steps. The method monitors the reaction process through GC and TLC, so that the cinnarizine yield is greatly enhanced up to over 85%. At the same time, the purity of the product of each reaction step is also high.

Description

technical field [0001] The invention relates to the field of medicine preparation methods, in particular to a new method for synthesizing cinnarizine. Background technique [0002] Cinnarizine is a calcium channel antagonist, which prevents calcium ions from entering vascular smooth muscle cells, dilates blood vessels, and improves circulation significantly. Moreover, it has an antagonistic effect on various vasoconstrictor substances, can relieve vasospasm, and has the effect of preventing vascular embrittlement at the same time. Clinically, cinnarizine is mainly used in the treatment of cerebrovascular disorders and peripheral vascular diseases such as cerebral embolism, cerebral thrombosis, cerebral arteriosclerosis, cerebral circulatory insufficiency caused by hypertension, cerebral hemorrhage and subarachnoid hemorrhage recovery period, traumatic brain injury sequelae. It is also effective for mental neuropathy and coronary arteriosclerosis caused by cerebral circulat...

Claims

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Application Information

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IPC IPC(8): C07D295/03C07D295/023
Inventor 王建军关建通李显焕肖鸿江晓漫
Owner 珠海保税区丽珠合成制药有限公司
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