|
【结 构 式】 
|
【药物名称】Disalazine, VUFB-17259 【化学名称】2-Acetoxy-5-[4-[N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenylazo]benzoic acid 【CA登记号】146404-38-8 【 分 子 式 】C21H19N5O6S 【 分 子 量 】469.47948 |
【开发单位】Res. Inst. Pharmacy Biochemistry (VUFB) (Originator) 【药理作用】Antiarthritic Drugs, IMMUNOMODULATING AGENTS, Immunosuppressants, TREATMENT OF MUSCULOSKELETAL & CONNECTIVE TISSUE DISEASES |
合成路线1
Diazotization of 4-[N-(4,6-dimethyl-2-pyrimidinyl)sulfamoyl]aniline (I) by means of sodium nitrite in diluted hydrochloric acid gives a corresponding diazonium salt (II), which is then reacted with salicylic acid (III) to afford the 2-hydroxy intermediate (IV). Disalazine is obtained by the reaction of (IV) with acetic anhydride or acetyl chloride.
| 【1】 Kejha, J.; et al.; Azo compounds of sulfonamides and hydroxy benzoic acids. Czech. Appl. 6722-87 . |
| 【2】 Kejha, J.; et al.; 5-((4-(4,6-Dimethyl-2-pyrimidinylsulfamoyl)phenyl)azo)acetylsalicylic acid. Czech Appl 1426-91 (1991); Eur Pat Appl 91 117 064.5 . |
| 【3】 Kuchar, M.; Disalazine. Drugs Fut 1992, 17, 2, 98. |
| 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) | 15238 | Sulfamethazine; 4-amino-N-(4,6-dimethyl-2-pyrimidinyl)benzenesulfonamide | 57-68-1 | C12H14N4O2S | 详情 | 详情 |
| (II) | 15239 | 4-[[(4,6-dimethyl-2-pyrimidinyl)amino]sulfonyl]benzenediazonium chloride | C12H12ClN5O2S | 详情 | 详情 | |
| (III) | 15240 | 2-Hydroxybenzoic acid; Salicylic acid | 69-72-7 | C7H6O3 | 详情 | 详情 |
| (IV) | 15241 | 5-[(E)-2-(4-[[(4,6-dimethyl-2-pyrimidinyl)amino]sulfonyl]phenyl)diazenyl]-2-hydroxybenzoic acid | C19H17N5O5S | 详情 | 详情 |
Extended Information