ZD-4190
N-(4-溴-2-氟苯基)-7-[2-(1H-1,2,3-三唑-1-基)乙氧基]-6-甲氧基喹喕啉-4-盐酸胺Chemical Name: N-(4-Bromo-2-fluorophenyl)-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]-6-methoxyquinazoline-4-amine hydrochloride
CAS No. 257938-36-6
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:Quinazolinone (III) was prepared by treatment of aminobenzamide (I) with Gold's reagent (II) in refluxing dioxan.Subsequent chlorination using thionyl chloride gave chloroquinazoline (IV).Nucleophilic displacement of the chlorine atom of (IV) with 4-bromo-2-fluoroaniline (V) yielded the anilinoquinazoline (VI).The benzyl group of (VI) was then cleaved with trifluoroacetic acid,and the resulting hydroxyquinazoline (VII) was finally coupled with (hydroxyethyl)triazole (VIII) using DEAD and PPh3 to furnish the title compound.
📌 参考资料/链接：
参考文献标题:Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors
文献作者:Hennequin,L.F.; Thomas,A.P.; Johnstone,C.; Stokes,E.S.; Lohmann,J.J.; Ogilvie,D.J.; Dukes,M.; Wedge,S.R.; Curwen,J.O.; Kendrew,J.; Lambert-van der Brempt,C.
参考来源:J Med Chem 1999,42(26),5369