以4-(3-氯-4-甲氧基苄基氨基)-2-[(2S)-2-羟甲基-1-吡咯烷基]-5-嘧啶羧酸乙酯为原料,在VDMSO∶VTHF=1∶1的混合溶液中,水解成酸后,与不同的胺反应,合成了8种未见文献报道的阿伐那非类似物.所合成的产物经^1H NMR、^13C NMR、ESI-MS得到验证.
The 8 kinds of no literature reports of avanafil analogues were synthesized by amidation of amines and hydrolyzate of 4-[( 3-chloro-4-methoxybenzyl) amino]-2-[( 2S)-2-hydroxymethyl-1-pyrrolidinyl]-5-pyrimidineethylformate( 1),which hydrolyzed in mixed solvent( VDMSO∶ VTHF= 1 ∶ 1). Their structure was characterized by1 H NMR,13 C NMR and ESI-MS.