Refining method for avanafil

A technology of avanafil and refining method, which is applied in the field of medicine, can solve the problems of poor dissolution effect and insufficient dissolution rate, and achieve the effects of high purity and yield, easy operation and good economic benefits
CN106336401AActive Publication Date: 2017-01-18SHANDONG CHENGCHUANG PHARMA R&D
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG CHENGCHUANG PHARMA R&D
Publication Date
2017-01-18

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Abstract

The invention discloses a refining method for avanafil. An avanafil bulk drug prepared by using the refining method has a particle size of no more than 30 [mu]m; so in the process of drying, an organic solvent can be easily volatilized and solvent residues are low in amount. The refining method comprises the following concrete steps: adding a crude avanafil product into an organic solvent and carrying out heating to a reflux state; after complete dissolving of solids, carrying out standing for cooling to 40 to 20 DEC C; then carrying out stirring for cooling to 10 to -10 DEG C and maintaining the temperature for 1 to 3 h; carrying out filtering; and subjecting a filter cake obtained in the previous step to vacuum drying. The organic solvent is a combination of two solvents, wherein one solvent is a strongly polar solvent and the other solvent is a moderately polar or non-polar solvent.
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Description

technical field

[0001] The invention relates to a refining method, in particular to a refining method of avanafil. It belongs to the field of medical technology. Background technique

[0002] Avanafil (Avanafil) is authorized by Mitsubishi Tanabe Pharmaceutical Co., Ltd. of Japan and developed by American Vefors Pharmaceuticals for the treatment of male erectile dysfunction. Avanafil is an oral, fast-acting, highly selective phosphodiesterase-5 (PDE-5) inhibitor, which can inhibit the metabolism of cyclic guanosine monophosphate in the body, thereby enhancing the relaxation of smooth muscle and reducing blood flow in the penis. Increased flow, which in turn aids in an erection. Its chemical structural formula is as follows:

[0003]

[0004] Chinese patent application CN103819460A discloses a process for refining avanafil, the method includes the following steps:

[0005] 1) Add the crude product of avanafil into a reaction kettle containing dichloromethane, stir and ...

Claims

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