PD-159790
Chemical Name: N-(1-Ethylpiperidin-3-yl)-N-[6-iodo-2-(trifluoromethyl)quinazolin-4-yl]amine
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:The cyclization of 2-amino-5-iodobenzoic acid (I) with an excess of refluxing trifluoroacetic anhydride (II) by means of triethylamine gives 6-iodo-2-(trifluoromethyl)-3,1-benzoxazin-4-one (III),which is treated with conc.aqueous NH4OH to afford 6-iodo-2-(trifluoromethyl)quinazolin-4(3H)-one (IV).The reaction of (IV) with refluxing POCl3 yields 4-chloro-6-iodo-2-(trifluoromethyl)quinazoline (V),which is finally condensed with 1-Ethylpiperidine-3-amine (VI) by means of triethylamine in ether.
📌 参考资料/链接:
参考文献标题:Quinazolines as inhibitors of endothelin converting enzyme
文献作者:Ahn,K.; Cheng,X.-M.; Doherty,A.M.; Elslager,E.F.; Kornberg,B.; Lee,C.; Leonard,D.; Nikam,S.S.; Werbel,L.M.(Pfizer Inc.)
参考来源:EP 0799221; JP 1998510834; US 5658902; WO 9619474