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Process for preparing bis-phenyl fluorozine

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: 2007-07-18
HEBEI MEDICAL UNIVERSITY
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  • Summary
  • 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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Example 1: The best preparation method of difenfluzine, including the following steps:

[0014] 1) Prepare by reacting 104 grams of γ-butyrolactone with 108 grams of thionyl chloride in the presence of 4 grams of anhydrous zinc chloride as a catalyst to obtain 114 grams of γ-chlorobutyryl chloride (boiling point 85° / 8666Pa), Reverse copy and take; 2) Then mix an appropriate amount of solvent 840ml of dichloromethane, 134g of fluorobenzene, 196.8g of aluminum chloride, cool to below 8℃, add 196.8γ-chlorobutyryl chloride dropwise, and stir at 8-10℃ 1 hour, stirring at room temperature for 6 hours, standing overnight, ice-decomposition, the water layer was extracted with 3*150ml dichloromethane, dried with calcium chloride, and then dichloromethane was distilled off, collected by distillation under reduced pressure at 156-158℃ / With the 4533Pa fraction, 248 grams of γ-chloro-4-fluorobenzene-1-butanone was obtained. 3) Use 63 g of benzyl alcohol to react with 300 ml of concentr...

Embodiment 2

[0015] Example 2-Calcium antagonistic properties: using classic and most suitable rabbit aortic ring specimens for studying calcium antagonists, using high potassium (KCL) to depolarize the open voltage-dependent calcium channel, using norepinephrine (NE ) Open receptor-gated calcium channels and observe the effect of dipfluzine on these two channels. It was found that the relaxation effect of dipfluzine on vasoconstriction caused by KCL and NE is similar to cinnarizine in nature, but its blocking voltage-dependent calcium channel effect is 4 times stronger than that of cinnarizine.

Embodiment 3

[0016] Example 3-Selective expansion of blood vessels: The isolated porcine arterial ring experiment was used to compare the effects of difenfluzine on the contraction of the isolated porcine basilar artery, coronary and radial arteries caused by KCL. It was found that difenfluzine inhibits KCL. Isolated porcine basilar artery, coronary artery and radial artery contracted PD 2 Respectively 5.7+0.6 (n=6), 5.4+_0.4 (n=6) and 4.6+_0.5 (n=5), that is, the selectivity to the basilar artery is the highest, and it is significantly stronger than cinnarizine ( 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 diphenfluazine. Background technique [0002] Cardiovascular and cerebrovascular diseases pose a serious threat to human health and even life safety. For many years, cardiovascular and cerebrovascular diseases are one of the diseases with the highest mortality among various diseases. In order to solve the patient's pain and save the patient's life, people have paid a great price to make various attempts. Therefore, the search for 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 pharmaceutical industries are particularly concerned. Although many drugs for the treatment of such diseases have appeared, how to improve their efficacy, reduce the dosage of drugs, and enhance the effects of drugs has been under research. Since intracellular calcium overload is considered to be the last common pathway...

Claims

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Application Information

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