Avanafil

A technology of ivanafil and intermediates, applied in the field of drug synthesis, can solve the problems of affecting product yield, high synthesis cost, long synthesis time and the like
CN103483323AInactive Publication Date: 2014-01-01SUZHOU UUGENE BIOPHARMA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SUZHOU UUGENE BIOPHARMA
Publication Date
2014-01-01
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides an avanafil intermediate A and an avanafil intermediate B, and a synthetic method of the avanafil intermediates A and B and avanafil. The synthetic method of the avanafil comprises the following steps: reacting a compound with the formula (I) with 2-methylaminopyrimidine at a temperature ranging from -10 DEG C to 5 DEG C to obtain the avanafil intermediate A; agitating the avanafil intermediate A with 3-chloro-4-methoxybenzylamine at the temperature ranging from 0 DEG C to 3 DEG C and reacting for 0.2-0.4 hour to obtain the avanafil intermediate B; and agitating the avanafil intermediate B with L-prolinol at the room temperature and reacting for 18-22 hours to obtain the avanafil. The structural formulas of the avanafil intermediates A and B and the compound with the formula (I) are shown in the specification. The avanafil intermediates A and B provided by the invention are simple in structure and good in product quality; the cost of the synthetic method is low; the synthetic route of the whole process is short and reaction steps are few, so that the reaction time is shortened and the yield and the purity of the avanafil intermediates A and B, and the avanafil are also improved.
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Description

technical field

[0001] The invention relates to an ivanafil intermediate, a synthesis method thereof, and a synthesis method of ivanafil, and belongs to the technical field of medicine synthesis. Background technique

[0002] Avanafil, whose chemical name is 4-[(3-chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N -(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide, the chemical formula is:

[0003]

[0004] Evanafil is a potent and highly selective phosphodiesterase 5 (PDE5) inhibitor, a research project transferred by Vivus from Mitsubishi Tanabe Pharmaceutical Co., Ltd., Japan, for the treatment of male erectile dysfunction (ED) . Data from clinical trials showed that Avanafil treated adequately for erections, a higher rate of vaginal penetration, a higher rate of adequately prolonged erections, and a higher rate of successful completion of intercourse with Avanafil compared with placebo. In addition to oral dosage forms, Vivus is also developing a urin...

Claims

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