【药物名称】
化学结构式(Chemical Structure):
参考文献No.46121
标题:Antibacterial quinazoline cpds.
作者:Guinosso, C.J.; Cook, P.D.; Kung, P.-P. (Isis Pharmaceuticals, Inc.)
来源:US 6156758
合成路线图解说明:

Palladium-catalyzed coupling of 4-amino-1-benzylpiperidine (I) with tert-butyl 4-bromobenzoate (II) afforded the anilinopiperidine derivative (III). Removal of the benzyl protecting group of (III) to give (IV) was achieved by transfer hydrogenolysis in the presence of ammonium formate and Pd/C. Piperidine (IV) was then coupled with 4-amino-2-chloro-6,7-dimethoxyquinazoline (V) in hot isoamyl alcohol yielding piperidino quinazoline (VI). The title carboxylic acid was finally obtained by acidic deprotection of tert-butyl ester of (VI).

参考文献No.555745
标题:Structure-activity relationships of novel 2-substituted quinazoline antibacterial agents
作者:Kung, P.-P.; Casper, M.D.; Cook, K.L.; Wilson-Lingardo, L.; Risen, L.M.; Vickers, T.A.; Ranken, R.; Blyn, L.B.; Wyatt, J.R.; Cook, P.D.; Ecker, D.J.
来源:J Med Chem 1999,42(22),4705
合成路线图解说明:

Palladium-catalyzed coupling of 4-amino-1-benzylpiperidine (I) with tert-butyl 4-bromobenzoate (II) afforded the anilinopiperidine derivative (III). Removal of the benzyl protecting group of (III) to give (IV) was achieved by transfer hydrogenolysis in the presence of ammonium formate and Pd/C. Piperidine (IV) was then coupled with 4-amino-2-chloro-6,7-dimethoxyquinazoline (V) in hot isoamyl alcohol yielding piperidino quinazoline (VI). The title carboxylic acid was finally obtained by acidic deprotection of tert-butyl ester of (VI).

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