Patent ID: 9593101
Date: 2017-03-14
CPC Classifications: C07D

Claim:
1. A method for preparing avanafil, with the chemical name (S)-4-[(3-chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidylmethyl)-5-pyrimidinecarboxamide (I), Wherein the said preparation method comprises the following steps: using cytosine as raw material, the cytosine and 3-chlorine-4-methoxybenzyl halogen (III) have a substitution reaction to produce N-(3-chloro-4-methoxybenzyl)cytosine (V) which then has a condensation reaction with S-hydroxymethyl pyrrolidine (II) to produce 4-[(3-chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]pyrimidine (VI). After halogenation reaction, 4-[(3-chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]pyrimidine (VI) and side chain N-(2-methylpyrimidine)methanamide (IV) have an addition reaction to prepare avanafil (I).