新产品编号:1133221

Chemical Name: (?-(2R*,5Z,9S*,10S*,16R*)-9-[N-[2-(1-Pyrrolidinyl)ethyl]carbamoyloxy]-10,2,10-(epoxymetheno)-1-benz[b]azacyclododeca-5-ene-3,7-diyne-1-carboxylic acid 4-chlorophenyl ester hydrochloride,mixture with the (2R*,5Z,9R*,10S*,16R*)-isomer (2:1)
项目整合开发状态: Preclinical
项目研究机构: Sanwa (Originator)
合成路线:Enediyne compound (I) as an unseparable 2:1 mixture of diastereoisomers was hydrolyzed with barium hydroxide in methanol-dichloromethane at 0 C to provide a mixture of alcohols (II),which were immediately converted into carbonyl imidazole intermediates (III) by treatment with carbonyldiimidazole (CDI) and 4-(dimethylamino)pyridine (DMAP) in cold dichloromethane.Reaction of (III) with an excess of 2-(1-pyrrolidinyl)ethylamine (IV) in dichloromethane at 0 C yielded a 2:1 mixture of diastereoisomeric carbamates,which on treatment with 0.01 M HCl gave the corresponding hydrochlorides.