Sepimostat mesilate, TO-187, FUT-187
6-(氨基亚胺甲基)-2-萘基4-((4,5-二氢-1H-咪唑-2-基)氨基苯甲酸酯二甲烷磺酸盐司匹司他Chemical Name: 4-(4,5-Dihydro-1H-imidazol-2-ylamino)benzoic acid 6-amidinonaphthalen-2-yl ester dimethanesulfonate; 6-[4-(2-Imidazolidinylideneamino)benzoyloxy]naphthalene-2-carboxamidine dimethanesulfonate
CAS No. 103926-82-5, 103926-81-4 (diHCl), 103926-64-3 (free base)
项目整合开发状态: Phase III
项目研究机构: Torii (Originator), Taiho (Licensee)
合成路线:Esterification of 4-(4,5-dihydro-1H-imidazol-2-ylamino)benzoic acid methanesulfonate (I) with 6-amidino-2-naphthol methanesulfonate (II) by means of dimethylaminopyridine (DMAP) and dicyclohexylcarbodiimide (DCC) in dry pyridine.
📌 参考资料/链接：
参考文献标题:Novel amidine cpds
文献作者:Fujii,S.; Okutome,T.; Nakayama,T.; Nunomura,S.; Sudo,K.; Watanabe,S.; Kurumi,M.; Aoyama,T.(Torii Pharmaceutical Co.,Ltd.)
参考来源:AU 8545492; EP 0190356; ES 8607218; US 4777182; US 4820730; WO 8600893
📄 详细内容
合成路线:Esterification of 4-(4,5-dihydro-1H-imidazol-2-ylamino)benzoic acid methanesulfonate (I) with 6-amidino-2-naphthol methanesulfonate (II) by means of dimethylaminopyridine (DMAP) and dicyclohexylcarbodiimide (DCC) in dry pyridine.
参考文献标题:Synthesis and structure-activity study of protease inhibitors.V.Chemical modification of 6-amidino-2-naphthyl 4-guanidinobenzoate
文献作者:Nakayama,T.; Taira,S.; Ikeda,M.; Ashizawa,H.; Oda,M.; Arakawa,K.; Fujii,S.
参考来源:Chem Pharm Bull 1993,41(1),117-25
合成路线:Esterification of 4-(4,5-dihydro-1H-imidazol-2-ylamino)benzoic acid methanesulfonate (I) with 6-amidino-2-naphthol methanesulfonate (II) by means of dimethylaminopyridine (DMAP) and dicyclohexylcarbodiimide (DCC) in dry pyridine.
参考文献标题:Sepimostat Mesylate
文献作者:Graul,A.; Leeson,P.; Castar,J.
参考来源:Drugs Fut 1997,22(5),502