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新产品编号:2367181

Chemical Name: N-(4-Chlorophenyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Originator), Millennium (Originator)
合成路线:The title urea derivative was synthesized by condensation of 6,7-dimethoxy-4-piperazinylquinazoline (I) with 4-bromophenyl isocyanate (II) in refluxing ethanol.

合成路线:The condensation of 6,7-dimethoxy-4-(1-piperazinyl)quinazoline (I) with 4-bromophenylamine (II) by means of CDI or triphosgene gives the target piperazine-1-carboxamide.Alternatively,the reaction of 4-bromophenylamine (II) with 4-nitrophenyl chloroformate (III) by means of TEA gives the carbamate (IV),which is finally condensed with the quinazoline (I) in hot NMP to yield the target piperazine-1-carboxamide.

合成路线:The target piperazine-1-carboxamide has been obtained by several different methods:1.- The condensation of 6,7-dimethoxy-4-(1-piperazinyl)quinazoline (I) with 4-chlorophenyl isocyanate (II) in DMF gives the target compound.2.- The condensation of 6,7-dimethoxy-4-(1-piperazinyl)quinazoline (I) with 4-chlorophenylamine (III) by means of CDI or triphosgene also gives the target piperazine-1-carboxamide.3.- The reaction of 4-chlorophenylamine (III) with 4-nitrophenyl chloroformate (IV) by means of TEA gives the carbamate (V),which is finally condensed with the quinazoline (I) in hot NMP to yield the target piperazine-1-carboxamide.
📌 参考资料/链接:
参考文献标题:Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation.1.Synthesis,structure-activity relationship,and biological effects of a new class of quinazoline derivatives
文献作者:Matsuno,K.; Ichimura,M.; Nakajima,T.; Tahara,K.; Fujiwara,S.; Kase,H.; Ushiki,J.; Giese,N.A.; Pandey,A.; Scarborough,R.M.; Lokker,N.A.; Yu,J.C.; Irie,J.; Tsukuda,E.; Ide,S.-i.; Oda,S.; Nomoto,Y.
参考来源:J Med Chem 2002,45(14),3057