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【结 构 式】

【药物名称】Troxipide, KU-54, Aplace

【化学名称】(±)-3-(3,4,5-Trimethoxybenzamido)piperidine

【CA登记号】30751-05-4

【 分 子 式 】C15H22N2O4

【 分 子 量 】294.35359

【开发单位】Kyorin (Originator)

【药理作用】Antiulcer Drugs, GASTROINTESTINAL DRUGS

合成路线1

The condensation of 3,4,5-trimethoxybenzoyl chloride (I) with 3-aminopyridine (II) by means of pyridine in benzene gives 3-(3,4,5-trimethoxybenzamido)pyridine (III), which is hydrogenated with H2 over Pd/C in ethanol-water-HCl.

1 Irikura, T.; et al.; Benzoylamino substituted 1-benzoylpiperidines. US 3647805 .
2 Irikura, T.; Kasuga, K.; New antiulcer agents. 1. Syntheses and biological activities of 1-acyl-2-, -3- and -4-substituted benzamidopiperidines. J Med Chem 1971, 14, 4, 357-361.
3 Blancafort, P.; Castaner, J.; Dharma, A.P.; Serradell, M.N.; KU-54. Drugs Fut 1979, 4, 12, 882.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 13571 3,4,5Ttrimethoxybenzoyl chloride 4521-61-3 C10H11ClO4 详情 详情
(II) 33327 3-Pyridinylamine; 3-Aminopyridine; 3-Pyridinamine 462-08-8 C5H6N2 详情 详情
(III) 33326 3,4,5-trimethoxy-N-(3-pyridinyl)benzamide C15H16N2O4 详情 详情
Extended Information