E-90/007, KW-2149, KT-6149

Chemical Name: 7-N-[2-[[2-(gamma-L-Glutamylamino)ethyl]dithio]ethyl]mitomycin C; (1aalpha,8balpha)-8beta-(Carbamoyloxymethyl)-6-[2-[2-(gamma-L-glutamylamino)ethyldithio]ethylamino]-8aalpha-methoxy-5-methyl-1,1a,2,4,7,8,8a,8b-octahydroazirino[2,'3,':3,4]pyrrolo[1,2-a]indole-4,7-dione; 7-N-[2-[[2-(N5-L-Glutamylamino)ethyl]dithio]ethyl]mitomycin C; [1aS-(1aalpha,8beta,8aalpha,8balpha)]-N-[2-[[2-[[8-[[(Aminocarbonyl)oxy]methyl]-1,1a,2,4,7,8,8a,8b-octahydro-8a-methoxy-5-methyl-4,7-dioxoazirino[2',3':3,4]pyrrolo[1,2-a]indol-6-yl]amino]ethyl]dithio]ethyl]-L-glutamine
CAS No. 118359-59-4
项目整合开发状态: Phase II
项目研究机构: Kyowa Hakko (Originator)
合成路线:The condensation of mitomycin A (I) with 2-(2-pyridyldithio)ethylamine (II) by means of triethylamine in methanol gives 7-N-[2-(2-pyridyldithio)ethyl]mitomycin C (III),which is then allowed to react with gamma-L-glutamylcysteamine (IV) in methanol.The gamma-L-glutamylcysteamine (IV) is obtained by deprotection of N,N'-bis[N-benzyloxycarbonyl-gamma-(alpha-benzyl)-L-glutamyl]cystamine (V) with anisole and trifluoroacetic acid giving the deprotected cystamine (VI),which is then reduced to the cysteamine (IV) with ethyl mercaptane.