Enzastaurin hydrochloride, LY-317615.2HCl, 317615.2HCl
3-(1-甲基-1H-吲哚-3-基)-4-[1-[1-(2-吡啶甲基)-4-哌啶基]-1H-吲哚-3-基]-1H-吡咯-2,5-二酮二盐酸盐 恩扎妥林Chemical Name: 3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione dihydrochloride
CAS No. 359017-72-4, 365253-37-8, 170364-57-5 (free base), 359017-79-1 (monoHCl)
项目整合开发状态: Phase II
项目研究机构: Lilly (Originator), National Cancer Institute (Codevelopment)
合成路线:Debenzylation of 1-benzyl-4-(1-indolyl)piperidine (I) with H2 and Pd(OH)2 leads to piperidine (II),which is further alkylated by 2-(bromomethyl)pyridine (III) to yield the pyridylmethyl piperidine (IV).Acylation of indole (IV) with oxalyl chloride produces the indoleglyoxylyl chloride (V).This is finally cyclized with the indolyl acetimidate (VI) in the presence of Et3N to produce the target bis-indolyl maleimide.
📌 参考资料/链接:
参考文献标题:Protein kinase C inhibitors
文献作者:Heath,W.F.H.Jr.; McDonald,J.H.III; Paal,M.; Rher,G.; Schotten,T.; Stenzel,W.(Eli Lilly and Company)
参考来源:EP 0817627; JP 1997507066; US 5545636; WO 9517182