以4‐（3‐氯‐4‐甲氧基苄基氨基）‐2‐[（2 S ）‐2‐羟甲基‐1‐吡咯烷基]‐5‐嘧啶羧酸乙酯为原料，合成了4‐（3‐氯‐4‐甲氧基苄基氨基）‐2‐[（2 S ）‐2‐羟甲基‐1‐吡咯烷基]‐N‐（2‐吡啶甲基）‐5‐嘧啶甲酰胺，研究了此种阿伐那非类似物的合成条件优化，考察了投料比、反应温度、反应时间等因素对产率的影响．获得较高产率的反应条件为n（C6H8N2）∶ n（C18H21ClN4O4）∶ n（EDCI）∶ n（HOBt）∶ n（Et3N）＝12．∶1∶12．∶12．∶2，在搅拌下，60℃反应6 h ，经过后处理，柱层析纯化，得到类白色固体产物，产率为843．％．所合成的产物经 FT‐IR、1 H NMR、13 C NMR、ESI‐MS得到验证．%4‐[(3‐chloro‐4‐methoxybenzyl)amino]‐2‐[(2S)‐2‐hydroxymethyl‐1‐pyrrolidinyl]‐N‐(2‐pyridinyl‐methyl)‐5‐pyrimidinecar‐boxamide was synthesized from 4‐[(3‐chloro‐4‐methoxy‐benzyl)amino]‐2‐[(2S)‐2‐hydroxymethyl‐1‐pyrrolidinyl]‐5‐pyrimidineethyl‐formate .The con‐ditions of feed ratio ,reaction temperature ,reaction time and other factors were optimized to prepare the yield . The reaction mixture was stirred at 60 ℃ temperature for 6h with n(C6H8N2)∶ n(C18H21ClN4O4)∶ n(EDCI):n(HOBt)∶ n(Et3N) = 1 2.∶1∶1 2.∶1 2.∶2 .Af‐ter column chromatography purification ,the product was obtained as white solid ,with the yield of 84 3.% .Its structure was characterized by FT‐IR ,1 H NMR ,13C NMR and ESI‐MS .
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