KRN-633-药物合成数据库

【药物名称】KRN-633

化学结构式(Chemical Structure):

参考文献No.	44408
标题:	Quinoline derivs. and quinazoline derivs.
作者:	Kubo, K.; Fujiwara, Y.; Isoe, T. (Kirin Brewery Co., Ltd.)
来源:	EP 1153920; WO 0043366

合成路线图解说明: 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No.	661728
标题:	Synthesis and structure-activity relationship of quinazoline-urea derivatives as novel orally active VEGF tyrosine kinase selective inhibitors
作者:	Kubo, K.; Iwakubo, M.; Fujiwara, Y.; et al.
来源:	Proc Am Assoc Cancer Res 2002,43Abst 913

合成路线图解说明: 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.