BKM-570
苯丙酰胺,4-[(2,6-二氯苯基)甲氧基]-α-[[1-氧基-3-(2,3,4,5,6-五氟苯)-2-丙烯-1-基]氨基]-N-(2,2,6,6-四甲基-4-哌啶基)-,(αS)-Chemical Name: O-(2,6-Dichlorobenzyl)-N2-[3-(pentafluorophenyl)-2-propenoyl]-N1-(2,2,6,6-tetramethylpiperidin-4-yl)-L-tyrosinamide
CAS No. 259885-54-6, 259886-28-7 (hydrochloride), 259886-27-6 (trifluoroacetate)
项目整合开发状态: Preclinical
项目研究机构: University of Colorado (Originator)
合成路线:N-Boc-O-(2,6-Dichlorobenzyl)-L-tyrosine (I) is coupled to 4-amino-2,2,6,6-tetramethylpiperidine (II) using BOP in DMF to provide amide (III).The N-Boc protecting group of (III) is then removed by trifluoroacetic acid,yielding amine (IV).This is finally acylated with pentafluorocinnamic acid (V) in the presence of BOP/i-Pr2NEt to furnish the title compound (1,2).
📌 参考资料/链接：
参考文献标题:Anti-cancer cpds.and methods related thereto
文献作者:Stewart,J.M.; Gera,L.; Chan,D.C.F.; York,E.; Bunn,P.
参考来源:WO 0011022
📄 详细内容
合成路线:N-Boc-O-(2,6-Dichlorobenzyl)-L-tyrosine (I) is coupled to 4-amino-2,2,6,6-tetramethylpiperidine (II) using BOP in DMF to provide amide (III).The N-Boc protecting group of (III) is then removed by trifluoroacetic acid,yielding amine (IV).This is finally acylated with pentafluorocinnamic acid (V) in the presence of BOP/i-Pr2NEt to furnish the title compound (1,2).
参考文献标题:Bradykinin-related compounds as new drugs for cancer and inflammation
文献作者:Stewart,J.M.; Gera,L..; Chan,D.C.; Bunn,P.A.Jr.; York,E.J.; Simkeviciene,V.; Helfrich,B.
参考来源:Can J Physiol Pharmacol 2002,80(4),275
产品链接: CAS No. 259885-54-6››