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Preparation method of cilostazol intermediate

A technology of cilostazol and intermediates, applied in the field of organic compound synthesis and pharmaceuticals, to achieve the effects of high product yield, mild reaction conditions and high purity

Pending Publication Date: 2020-07-28
HUNAN FURUI BIOPHARMA TECH CO LTD
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  • Description
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AI Technical Summary

Problems solved by technology

[0005] For the synthesis of an important intermediate of cilostazol, 1-(5-chloropentyl)-5-cyclohexyl-1H-tetrazole, there are few related documents disclosing its preparation method

Method used

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  • Preparation method of cilostazol intermediate
  • Preparation method of cilostazol intermediate
  • Preparation method of cilostazol intermediate

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Embodiment Construction

[0024] The technical solutions of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Apparently, the described embodiments are only some of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without creative efforts fall within the protection scope of the present invention.

[0025] As a preparation method of a cilostazol intermediate shown in the examples, the cilostazol intermediate is synthesized with cyclohexylamine and 5-chlorovaleraldehyde as starting materials;

[0026] The synthesis path is:

[0027]

[0028] Its preparation method comprises the following steps:

[0029] Q1. Synthesis of compound 1: react cyclohexylamine and 5-chloropentanal in an alcohol solvent to obtain compound 1, the reaction temperature is 90-120°C, and the reaction time is 8-10 hours; ...

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Abstract

The invention provides a preparation method of a cilostazol intermediate. Cyclohexylamine and 5-chlorovaleraldehyde are used as initial raw materials to synthesize a cilostazol intermediate and the cilostazol intermediate undergoes a three-step reaction to produce a high-purity cilostazol intermediate. The method has gentle reaction conditions, simple process, convenient operation, high purity ofthe obtained cilostazol intermediate, cheap and easily available raw materials, low cost, short steps of the whole reaction route, high product yield and high industrial production benefit, so that avaluable synthetic route is provided for preparation of cilostazol, good social and economic benefits can be brought, and the economic value potential is large.

Description

technical field [0001] The present invention relates to the technical field of organic synthesis and pharmacy, in particular to a method for preparing a cilostazol intermediate used in the preparation of cilostazol. Background technique [0002] Cilostazol, a quinolinone derivative, is a commonly used antiplatelet and anticoagulant drug in clinical practice. It belongs to phosphodiesterase (PDE) inhibitors and can inhibit the activity of phosphodiesterase in platelets and smooth muscle cells. Cilostazol can increase the concentration of cAMP in platelets and vascular smooth muscle, and is generally used for local ischemic diseases such as chronic arterial occlusive ulcers, pain and cold sensation. Cilostazol generally has the following uses: 1. Improve ischemic symptoms such as ulcers, limb pain, cold sensation and intermittent claudication caused by chronic arterial occlusive disease; 2. Adjuvant treatment of atherosclerosis, Takayasu, Thromboangiitis obliterans, limb isch...

Claims

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Application Information

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IPC IPC(8): C07D257/04
CPCC07D257/04
Inventor 鲁光英毕波周跃辉罗盼
Owner HUNAN FURUI BIOPHARMA TECH CO LTD
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