西地那非4-哌嗪位丁酸修饰衍生物的合成

Synthesis of Sildenafil Analogue Containing Butyric Acid Group in the 4-Piperazine Moiety

从原料5-(2-乙氧苯基)-1-甲基-3-丙基-1,6-二氢-7 H-吡唑并[4,3-d]嘧啶-7-酮开始,合成了西地那非4-哌嗪位丁酸修饰衍生物5-(2-乙氧基-5-(4-(3-羟羧基丙基)哌嗪基磺酰基)苯基)-1-甲基-3-丙基-1,6-二氢-7 H-吡唑并[4,3-d]嘧啶-7-酮,核磁、质谱、红外验证了其分子结构,高效液相检测纯度97.78%,总收率74.0%。

Sildenafil analogue containing butyric acid group in the 4-piperazine moiety, 5-（2-ethoxy-5-（4-（3- hydroxycarbonylpropyl） piperazinylsulfonyl） phenyl）-1-methyl-3-n-propyl-1,6-dihydro-7 H-pyrazolo [4,3-d] pyrimidin-7-one, was prepared from the starting material 5- （2-ethoxyphenyl）-1-methyl-3-n-propyl-1,6-di- hydro-7H-pyrazolo[4,3-d]pyrimidin-7-one. The molecular structure was identified with 1H NMR, LC-MS （MS） and IR. HPLC detection indicated that the purity of the product was 97.78%, and the total yield reached 74.0%.