合成路线:1) The condensation of a phenylpiperazine (I) with chloroethanol (II) gives compound (III) which,upon reaction with the acid chloride (IV),yields lobuprofen.
参考文献标题:Lobuprofen hydrochloride
文献作者:Carretero,J.M.; Alamo,C.; Mart韓,J.L.
参考来源:Drugs Fut 1988,13(4),314
合成路线:The reaction of ethyl 8-nitro-4-oxo-1-benzopyran-2-carboxylate (I) with ammonia in methanol gives the corresponding amide (II),which is dehydrated with POCl3 yielding 2-cyano-8-nitro-1-benzopyran-4-one (III).The cyclization of (III) with sodium azide by means of pyridinium chloride in hot DMF affords 8-nitro-2-(tetrazol-5-yl)-1-benzopyran-4-one (IV),which is hydrogenated with H2 over Pd/C in methanol - HCl giving 8-amino-2-(tetrazol-5-yl)-1-benzopyran-4-one (V).Finally,this compound is condensed with 4-(4-phenylbutoxy)benzoic acid (VI) by means of oxalyl chloride in dichloromethane-pyridine.
合成路线:2) The acid chloride (IV) is reacted with chloroethanol to give compound (V),which,upon condensation with a piperazine (I),yields lobuprofen.
参考文献标题:ONO-RS-411
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1988,13(4),317
产品链接: CAS No. 96128-90-4››