KRN-633
N-[2-氯-4-[(6,7-二甲氧基-4-喹唑啉基)氧基]苯基]-N'-丙基脲Chemical Name: N-[2-Chloro-4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl]-N'-propylurea
CAS No. 286370-15-8
项目整合开发状态: Preclinical
项目研究机构: Kirin Brewery (Originator)
合成路线:6,7-Dimethoxy-4-quinazolone (II) was prepared by condensation of methyl 4,5-dimethoxyanthranilate (I) with formamide at 160 C.Chlorination of (II) by means of phosphorus oxychloride provided the 4-chloro quinazoline (III).Substitution of the 4-chloro group of (III) by the sodium salt of 4-amino-3-chlorophenol (IV) gave rise to the quinazolinyl ether (V).Finally,condensation of amine (V) with triphosgene,followed by addition of n-propylamine furnished the title urea derivative.
📌 参考资料/链接：
参考文献标题:Quinoline derivs.and quinazoline derivs.
文献作者:Kubo,K.; Fujiwara,Y.; Isoe,T.(Kirin Brewery Co.,Ltd.)
参考来源:EP 1153920; WO 0043366
📄 详细内容
合成路线:6,7-Dimethoxy-4-quinazolone (II) was prepared by condensation of methyl 4,5-dimethoxyanthranilate (I) with formamide at 160 C.Chlorination of (II) by means of phosphorus oxychloride provided the 4-chloro quinazoline (III).Substitution of the 4-chloro group of (III) by the sodium salt of 4-amino-3-chlorophenol (IV) gave rise to the quinazolinyl ether (V).Finally,condensation of amine (V) with triphosgene,followed by addition of n-propylamine furnished the title urea derivative.
参考文献标题:Synthesis and structure-activity relationship of quinazoline-urea derivatives as novel orally active VEGF tyrosine kinase selective inhibitors
文献作者:Kubo,K.; Iwakubo,M.; Fujiwara,Y.; et al.
参考来源:Proc Am Assoc Cancer Res 2002,43Abst 913
产品链接: CAS No. 286370-15-8››