Cilazapril, Ro-312848, Inibace, Dynorm, Cilazil, Justor, Vascace, Inhibace

西拉普利 西拉普利 Chemical Name: (1S,9S)-9-[1(S)-Ethoxycarbonyl-3-phenylpropylamino]-10-oxoperhydropyridazine[1,2-a][1,2]diazepine-1-carboxylic acid
CAS No. 88768-40-5, 92077-78-6 (monohydrate)
项目整合开发状态: Launched-1990
项目研究机构: Roche (Originator), Chiesi (Licensee), Eisai (Licensee), Pliva (Licensee)
合成路线:The condensation of acyl chloride (I) with hexahydropyridazine (II) gives the corresponding amide (III),which is debenzylated with H2 over Pd/C and cyclized by means of SOCl2 to yield the pyridazinodiazepinedione (IV).Selective reduction of (IV) with borane in THF affords the pyridazinodiazepinone (V),which is treated with hydrazine to provide (1S,9S)-9-amino-10-oxoperhydropyridazino[1,2-a]azepine-1-carboxylic acid tert-butyl ester (VI).Finally,this compound is condensed with 4-phenyl-2(R)-(trifluoromethanesulfonyloxy)butyric acid ethyl ester (VII) and selectively hydrolyzed to afford the target carboxylic acid.