Process for preparing bis-phenyl fluorozine and its use as medicine in treatment of cardiovascular and cerebrovascular diseases

A technology of difluzine and benzhydrylpiperazine, which is applied in the field of preparation of difluzine, can solve problems such as heart damage and cerebrovascular stealing, and achieve the effects of increasing yield, simplifying process, and qualified quality

Inactive Publication Date: 2005-08-17
HEBEI MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It is known that flunarizine and nimodipine are the most widely used in the treatment of ischemic brain injury, but they have side effects such as heart damage, blood pressure drop and cerebrovascular "stealing" (Wu Mingyuan, Shi Yifu

Method used

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  • Process for preparing bis-phenyl fluorozine and its use as medicine in treatment of cardiovascular and cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1: the optimal preparation method of difluzine, comprises the steps:

[0016] 1) 104 grams of γ-butyrolactone and 108 grams of thionyl chloride are reacted in the presence of catalyzer 4 grams of anhydrous zinc chloride to obtain 114 grams of product γ-butyryl chloride (boiling point 85° / 8666Pa), Repeatedly take; 2) Then mix appropriate amount of solvent 840ml dichloromethane, 134g fluorobenzene, 196.8g aluminum chloride, cool to below 8°C, add dropwise 196.8 gamma-chloride butyryl chloride, stir at 8-10°C 1 hour, stirred at room temperature for 6 hours, left overnight, ice-thawed, the water layer was extracted with 3*150ml dichloromethane, dried with calcium chloride, then distilled dichloromethane, vacuum distillation collected 156-158℃ / The fraction of 4533Pa produced 248 grams of product gamma-chloro-4-fluorobenzene-1-butanone. 3) 55.4 grams of diphenylchloromethane (132-135°C / 160Pa) was obtained by reacting 63 grams of diphenylmethanol with 300ml of con...

Embodiment 2

[0017] Example 2-calcium antagonistic properties: using the classic, most suitable rabbit aortic ring specimen for the study of calcium antagonists, using high potassium (KCL) to depolarize and open voltage-dependent calcium channels, and using norepinephrine (NE ) to open receptor-gated calcium channels, and the effect of difluzine on these two channels was observed. It was found that the relaxation effect of difluzine on the vasoconstriction induced by KCL and NE is similar in nature to that of cinnarizine, but its blocking effect on voltage-dependent calcium channels is 4 times stronger than that of cinnarizine.

Embodiment 3

[0018] Example 3-selective dilation of blood vessels: using isolated porcine arterial ring experiments, compared the effects of difluzine on the constriction of isolated porcine basilar arteries, coronary arteries and radial arteries caused by KCL and found that difluzine inhibited the constriction caused by KCL PD of contraction of isolated porcine basilar, coronary and radial arteries 2 They are 5.7+_0.6 (n=6), 5.4+_0.4 (n=6) and 4.6+_0.5 (n=5), respectively, that is, the selectivity to the basilar artery is the highest, and it is significantly stronger than Guili Zine (PD 2 is 5.0+_0.4 n=6 p<0.55).

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Abstract

The present invention relates to the preparation process of diphenyl ofloxacin and its application in preparing medicine for treating cardiac and cerebral vascular diseases. The preparation process includes the following steps: A) preparing gamma-chloro-4-fluorobenzene-1-butanone through the reaction between gamma-butyrolactone and sulfoxide chloride to obtain gamma-butyryl chloride and the subsequent reaction in mixed solvent with catalyst; B) preparing benzhydryl piperazine through the reaction between diphenylcaabinol and concentrated hydrochloric acid to obtain diphenyl chloromethane, the subsequent reaction in mixed solvent with catalyst and filtering; and C) preparing the product diphenyl ofloxacin with proper amount of benzhydryl piperazine, gamma-chloro-4-fluorobenzene-1-butanone, solvent methyl isobutyl ketone and catalyst potassium iodide and potassium carbonate, and through mixing and reaction.

Description

technical field [0001] The invention relates to a preparation method of difluzine, and also relates to the application of the difluzine prepared by the preparation method in the preparation of medicines for preventing and treating cardiovascular and cerebrovascular diseases of mammals and humans. Background technique [0002] Cardiovascular and cerebrovascular diseases pose a serious threat to human health and even life safety. Cardiovascular and cerebrovascular diseases have been one of the diseases with the highest mortality rate in various diseases for many years. In order to solve the patient's suffering and save the patient's life, people have paid a great price to carry out various attempts. Therefore, seeking effective drugs for the treatment of cardiovascular and cerebrovascular diseases has always attracted the attention of people from all walks of life. The chemical and medical circles are particularly concerned. Although many medicines for the treatment of thes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61P9/00C07D295/108
Inventor 王永利陈子明胞春和张永健
Owner HEBEI MEDICAL UNIVERSITY
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