EKI-785, CL-387785

N-[4-[(3-溴苯基)氨基]-6-喹唑啉基]-2-丁炔酰胺Chemical Name: N-[4-(3-Bromophenylamino)quinazolin-6-yl]-2-butynamide
CAS No. 194423-06-8
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:The reaction of 2-amino-5-nitrobenzoic acid (I) with N,N-dimethylformamide dimethylacetal (II) by heating at 100 C gives the formamidine (III),which is cyclized with 3-bromoaniline (IV) in refluxing acetic acid yielding 4-(3-bromophenyl)-6-nitroquinazoline (V).The reduction of (V) with Fe and acetic acid affords the amine (VI),which is finally acylated with 2-butynoic acid by means of isobutyl chloroformate and N-methylmorpholine in THF.