【结 构 式】 |
【药物名称】A-204176 【化学名称】N-[5-(1H-Imidazol-4-yl)-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide 【CA登记号】258527-44-5, 258526-38-4 (HCl), 258818-73-4 (R-isomer), 258526-39-5 (R-isomer, HCl salt), 258818-86-9 (S-isomer), 258526-40-8 (S 【 分 子 式 】C14H17N3O2S 【 分 子 量 】291.37449 |
【开发单位】Abbott (Originator) 【药理作用】RENAL-UROLOGIC DRUGS, Urinary Incontinence Therapy, alpha1A-Adrenoceptor Agonists |
合成路线1
Reaction of methanesulfonamide derivative (I) with 4-iodo-N,N-dimethyl-1H-imidazole-1-sulfonamide (I) and EtMgBr in CH2Cl2 followed by heating with diluted HCl affords compound (III), which is debenzylated and reduced by hydrogenation over Pd/C in MeOH.
【1】 Altenbach, R.J.; Holladay, M.W.; Carroll, W.A.; Meyer, M.D.; Kerwin, J.F. Jr.; Kolasa, T.; Rohde, J.; Khilevich, A. (Abbott Laboratories Inc.); Imidazoles and related cpds. as alpha1A agonists. WO 0007997 . |
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) | 44142 | N-benzyl-N-(5-oxo-5,6,7,8-tetrahydro-1-naphthalenyl)methanesulfonamide | C18H19NO3S | 详情 | 详情 | |
(II) | 44143 | 4-iodo-N,N-dimethyl-1H-imidazole-1-sulfonamide | C5H8IN3O2S | 详情 | 详情 | |
(III) | 44144 | N-benzyl-N-[5-(1H-imidazol-4-yl)-7,8-dihydro-1-naphthalenyl]methanesulfonamide | C21H21N3O2S | 详情 | 详情 |
Extended Information