【结 构 式】 |
【药物名称】 【化学名称】N-[1-(4-Fluorophenylsulfonyl)piperidin-4-yl]acetamide 【CA登记号】 【 分 子 式 】C13H17FN2O3S 【 分 子 量 】300.35444 |
【开发单位】Università degli Studi di Firenze (Originator) 【药理作用】Cognition Disorders, Treatment of, NEUROLOGIC DRUGS |
合成路线1
Acylation of 4-amino-1-benzylpiperidine (I) with acetyl chloride provides the amide (II). Subsequent debenzylation of (II) by transfer hydrogenation with ammonium formate in the presence of Pd/C yields the piperidine (III), which is finally acylated with 4-fluorobenzenesulfonyl chloride (IV) to give the corresponding sulfonamide.
【1】 Manetti, D.; Martini, E.; Ghelardini, C.; Dei, S.; Galeotti, N.; Guandalini, L.; Romanelli, M.N.; Scapecchi, S.; Teodori, E.; Bartolini, A.; Gualtieri, F.; 4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs. Bioorg Med Chem Lett 2003, 13, 14, 2303. |
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) | 34808 | 1-Benzyl-4-piperidinylamine; 1-Benzyl-4-piperidinamine; 4-Amino-1-benzylpiperidine | 50541-93-0 | C12H18N2 | 详情 | 详情 |
(II) | 64809 | N-[1-(phenylmethyl)-4-piperidinyl]acetamide | C14H20N2O | 详情 | 详情 | |
(III) | 64810 | N-(4-piperidinyl)acetamide | C7H14N2O | 详情 | 详情 | |
(IV) | 12292 | 4-Fluorobenzenesulfonyl chloride | 349-88-2 | C6H4ClFO2S | 详情 | 详情 |
Extended Information