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
View PDF5 Cites 4 Cited by
  • 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 a

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • New synthesis method of cinnarizine
  • New synthesis method of cinnarizine
  • New synthesis method of cinnarizine

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0043] Example 1

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

Example Embodiment

[0045] Example 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 until there is benzene reflux, start dripping benzyl chloride 9.0g, and react for 4h after dripping. Let stand to separate the lower layer of zinc chloride solution, add 180 ml of water to the upper layer, stir for 5 min, stand for 10 min, collect the organic phase, and spin-evaporate to obtain 9.5 g of diphenylmethane product, with a yield of 35% and a GC purity of 96%.

Example Embodiment

[0047] Example 3

[0048] Add 11mol / L aluminum chloride solution (15ml, 0.165mol) and benzene (30ml, 0.155mol) into a 250ml three-necked flask, stir and heat until there is benzene reflux, start dripping benzyl chloride 9.0g, and react for 4h after dripping. Let stand to separate the lower layer of zinc chloride solution, add 180 ml of water to the upper layer, stir for 5 min, stand for 10 min, collect the organic phase, and rotate to dry to obtain 20.6 g of diphenylmethane product, with a yield of 76% and a GC purity of 96%.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap