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【结 构 式】 
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【药物名称】 【化学名称】N-(5-Aminosulfonyl-1,3,4-thiadiazol-2-yl)-2-(N1-methylguanidino)acetamide trifluoroacetate 【CA登记号】 【 分 子 式 】C8H12F3N7O5S2 【 分 子 量 】407.35194 |
【开发单位】Università degli Studi di Firenze (Originator) 【药理作用】Antiglaucoma Agents, OCULAR MEDICATIONS, Ophthalmic Drugs, Carbonic Anhydrase Inhibitors |
合成路线1
The condensation of 5-amino-1,3,4-thiadiazol-2-sulfonamide (I) with the protected guanidinoacetic acid (II) by means of EDC in acetonitrile gives the corresponding amide (III), which is then deprotected with HCl in hot dioxane.
| 【1】 Mincione, F.; Briganti, F.; Mincione, G.; Scozzafava, A.; Menabuoni, L.; Supuran, C.T.; Carbonic anhydrase inhibitors: Synthesis of water-soluble, aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route. J Med Chem 1999, 42, 18, 3690. |
| 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) | 38281 | 5-amino-1,3,4-thiadiazole-2-sulfonamide | C2H4N4O2S2 | 详情 | 详情 | |
| (II) | 38282 | 2-[[imino[(tritylsulfanyl)amino]methyl](methyl)amino]acetic acid | C23H23N3O2S | 详情 | 详情 | |
| (III) | 38283 | N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]-2-[[imino[(tritylsulfanyl)amino]methyl](methyl)amino]acetamide | C25H25N7O3S3 | 详情 | 详情 |
Extended Information