新产品编号:744049

Chemical Name: 2-(4-Fluorophenyl)-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one
CAS No. 283172-76-9
项目整合开发状态: Preclinical
项目研究机构: Agouron (Originator), Cancer Research UK (Originator)
合成路线:Condensation of methyl indole-4-carboxylate (I) with 2-nitroethyl acetate (II) produced the 3-nitroethyl indole (III).After reduction of the nitro group to amine (IV) using Zn and HCl,cyclization under basic conditions gave rise to lactam (V).Electrophilic bromination of (V) employing pyridinium tribromide furnished (VI).Finally,Suzuki coupling of bromide (VI) with 4-fluorobenzeneboronic acid (VII) yielded the title compound.
📌 参考资料/链接:
参考文献标题:Tricyclic inhibitors of poly(ADP-ribose) polymerases
文献作者:Thoresen,L.H.; Webber,S.E.; Tikhe,J.; Canan-Koch,S.S.(Agouron Pharmaceuticals,Inc.; Cancer Research Campaign Technology Ltd.)
参考来源:EP 1140936; WO 0042040