Novel intermediate used for preparation of avanafil and preparation method thereof

A technology of avanafil and intermediates, which is applied in the field of key intermediates of avanafil, can solve the problems of cumbersome post-processing, etc., and achieve the effect of being beneficial to purification, easy to purify, and reducing the use of column chromatography
CN104059025AActive Publication Date: 2014-09-24REGENEX PHARMA LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
REGENEX PHARMA LTD
Publication Date
2014-09-24

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Abstract

The invention provides a novel intermediate IV which is used for preparation of avanafil. The intermediate has a general formula IV as described in the specification; and in the general formula IV, R represents a C1-20 alkylsulfinyl group or a C1-20 alkylsulfonyl group. The intermediate has high purity, is suitable for industrial production and can be subjected to a one-step chemical reaction to prepare avanafil. The invention also provides a preparation method for the intermediate and a method for preparing avanafil from the intermediate.
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Description

technical field

[0001] The present invention relates to the key intermediate of avanafil, namely 4-(3-chloro-4-methoxybenzylamino)-2-Ryl-N-(2-pyrimidinylmethyl)pyrimidine-5-carboxamide The preparation method and its application in the preparation of avanafil belong to the field of medicinal chemistry. Background technique

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

[0003]

[0004] Avanafil is a new drug for the treatment of erectile dysfunction produced by Vivus. It was approved by the FDA on April 27, 2012. It is compatible with Sildenafil (Pfizer), Tadalafil ( Tadalafil (Eli Lilly) and Vardenafil (Vardenafil, Bayer) have the same mechanism of action and are 5-phosphodiesterase (PED-5) inhibitors. Studies have shown that the onset time of the drug is only 15 minutes, far shorter than the 30-60 minutes rep...

Claims

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