摘要
以异喹啉、喹啉为原料,经季铵化、环合合成了2-芳基咪唑骈[2,1-a]异喹啉(Ⅰa,Ⅰb)及2-芳基咪唑骈[1,2-a]喹啉(Ⅱa,Ⅱb),并发现化合物(Ⅱ)可由喹啉季铵盐(V)在AcONH_4-AcOH-FeCl_3或NH_2OH·HCl-H_2O体系中直接环合制得.药理试验表明:上述化合物均有不同程度的口服抗早孕活性,其中以2-联苯基取代物活性较高.
2-Arylimidazo (2, 1-a) isoquinolines(Ia, Ib)and 2-arylimidazo (1,2-a)quinolines( Ⅱa、Ⅱb)were synthesized with isoquinoline or quinoline as the raw material, through quaterisation and subsequnt cyclization. A simple synthetic method for compounds(Ⅱ) with quinolium salts in AcONH_4-AcOH-FeCl_3 or NH_2OH·HCl-H_2O system was developed. These derivatives showed certain pregnancy terminating activity in aminal tests. Among them,2-biphenylyl group compounds exhibited more potent activity than the others.
关键词
喹啉类
化学合成
避孕药
Quinolines/chem syn
2-Arylimidazo (2
1-a)isoquinolines
Pregnancy termination activity
Contraceptives
postcoital
synthetic/chem syn
