AVANAFIL PREPARATION METHOD

摘要

Disclosed is a method for preparing avanafil (I) by using cytosine as the starting material. The preparation steps comprise: using cytosine as the raw material, and enabling the cytosine to react with side chain 3-chlorine-4-methoxybenzyl halogen, N-(2-methylpyrimidine) methanamide and S-hydroxymethyl pyrrolidine, to prepare the target product avanafil (I). For the preparation method, the raw material is easily obtained, and the process is simple, economical, and environmentally friendly, so the method meets the requirement of industrial boost.

主权项

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).