|
【结 构 式】 
|
【药物名称】REC-15/3079 【化学名称】N-[2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl]-N-(2-nitrophenyl)cyclohexanecarboxamide 【CA登记号】 【 分 子 式 】C26H34N4O4 【 分 子 量 】466.58528 |
【开发单位】Recordati (Originator) 【药理作用】RENAL-UROLOGIC DRUGS, Urinary Incontinence Therapy, 5-HT1A Antagonists |
合成路线1
The condensation of 1-(2-aminoethyl)-4-(2-methoxyphenyl)piperazine (I) with 2-chloronitrobenzene (II) by means of K2CO3 in refluxing butanol gives 1-(2-methoxyphenyl)-4-[2-(2-nitrophenylamino)ethyl]piperazine (III), which is finally condensed with cyclohexylcarbonyl chloride (IV) by means of TEA in dichloroethane to afford the target amide.
| 【1】 Leonardi, A.; Motta, G.; Testa, R.; Riva, C. (Recordati Industria Chimica e Farmaceutica SpA); 1-(N-Phenylaminoalkyl)-piperazine derivs. substd. at position 2 of the phenyl ring. EP 1000047; JP 2001512112; US 6399614; WO 9906384 . |
| 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) | 53508 | 2-[4-(2-methoxyphenyl)-1-piperazinyl]-1-ethanamine; 2-[4-(2-methoxyphenyl)-1-piperazinyl]ethylamine | n/a | C13H21N3O | 详情 | 详情 |
| (II) | 15248 | 1-chloro-2-nitrobenzene | 88-73-3 | C6H4ClNO2 | 详情 | 详情 |
| (III) | 53509 | N-{2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl}-N-(2-nitrophenyl)amine; N-{2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl}-2-nitroaniline | n/a | C19H24N4O3 | 详情 | 详情 |
| (IV) | 17220 | cyclohexanecarbonyl chloride; Cyclohexanecarboxylic acid chloride | 2719-27-9 | C7H11ClO | 详情 | 详情 |
Extended Information