TRK-851
Chemical Name: (4bS,8R,8aS,16bR)-7-(Cyclopropylmethyl)-11-fluoro-5,6,7,8,9,14,15,16b-octahydro-4,8-methano-8aH,13H-[1]benzofuro[2,3-a]dipyrido[4,3-b:3',2',1'-jk]carbazole-1,8a-diol
CAS No. 189015-24-5, 189015-25-6 (monomethanesulfonate)
项目整合开发状态: Phase I
项目研究机构: Toray (Originator), Mitsubishi Pharma (Codevelopment)
合成路线:The title polycyclic compound was synthesized by Fisher indolization of naltrexone (I) with 1-amino-6-fluoro-1,2,3,4-tetrahydroquinoline (II) in the presence of methanesulfonic acid in refluxing EtOH.
📌 参考资料/链接：
参考文献标题:Indole derivs.and medicinal use thereof
文献作者:Nagase,H.; Kawai,K.; Endo,T.; Ueno,S.; Maeda,M.; Sakami,S.(Toray Industries,Inc.)
参考来源:EP 0805157; US 5849731; WO 9711948
📄 详细内容
合成路线:The title polycyclic compound was synthesized by Fisher indolization of naltrexone (I) with 1-amino-6-fluoro-1,2,3,4-tetrahydroquinoline (II) in the presence of methanesulfonic acid in refluxing EtOH.
参考文献标题:Rational drug design and synthesis of opioid delta-receptor selective antagonist TRK-851 and its antitussive activity
文献作者:Maeda,M.; et al.
参考来源:20th Symp Med Chem (Dec 6 2000,Tokyo) 2000,Abst 1P-16
产品链接: CAS No. 189015-24-5››