摘要
以氢化钠为催化剂,对三氟甲基苯甲酸甲酯与乙酸乙酯在THF中经缩合反应制得中间体二羰基酯(1);1与盐酸胍经环合反应得6-[4-(三氟甲基)苯基]-4-羟基-2-氨基嘧啶(2);2与ɑ-溴代对氯苯乙酮进一步环合得咪唑并[1,2-a]嘧啶类化合物(3);3与三氯氧磷经氯代反应后再与胺经取代反应合成了3个新型的2-(4-氯苯基)-7-[4-(三氟甲基)苯基]咪唑并[1,2-a]嘧啶类化合物,其结构经1H NMR和IR表征。
6-[ （Trifluoromethyl） phenyl ] -4-hydroxyl-2-aminopyrimidine （2） was prepared by conden- sation of ethyl acetate with methyl 3-oxo-3-[4-（trifluoromethyl） phenyl] propanoate in THF using Nail as the catalyst. Three novel imidazo [ 1,2-a ] pyrimidine compounds were synthesized by eyclization of 2 with guanidine, and then cyclization with 2-bromo-l-（4-chlorophenyl）ethanone, chlorination with phosphoryl trichloride and aminization with amines. The structures were characterized by 1H NMR and IR.
出处
《合成化学》
CAS
CSCD
北大核心
2013年第6期679-682,共4页
Chinese Journal of Synthetic Chemistry
基金
国家"十二五"重大新药创制科技重大专项资助项目(2011ZX09102-007-02)
关键词
咪唑并[1
2-a]嘧啶
环合
氯代
胺化
合成
imidazo [ 1,2-a ] pyrimidine
cyclization
chlorination
aminization
synthesis
