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【结 构 式】 
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【药物名称】Lidofenin, 99Tcm-HIDA, Hepato-Scan 【化学名称】[N-(2,6-Dimethylphenyl)carbamoylmethylimino]diacetic acid technetium-99 【CA登记号】59160-29-1 【 分 子 式 】C14H18N2O5Tc 【 分 子 量 】393.30996 |
【开发单位】 【药理作用】DIAGNOSTIC AGENTS, Technetium Complexes |
合成路线1
Compound can be prepared in two related ways: 1) The acylation of 2,6-dimethylaniline (I) with chloroacetyl chloride (II) in acetic acid gives omega-chloro-2,6-dimethylacetanilide (III), which is then condensed with disodium salt of iminodiacetic acid (IV) in refluxing ethanol-water. 2) The reaction of (III) with ammonia in ethanol gives omega-amino-2,6-dimethylacetanilide (V), which is finally treated with chloroacetic acid (A) and NaOH in refluxing 95% ethanol.
| 【1】 Castaner, J.; Blancafort, P.; Serradell, M.N.; Paton, D.M.; Lidofenin. Drugs Fut 1979, 4, 5, 342. |
| 【2】 Callery, P.S.; et al.; Tissue distribution of technetium-99m and carbon-14 labeled N-(2,6-dimethylphenylcarbamoylmethyl)iminodiacetic acid. J Med Chem 1976, 19, 7, 962-964. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (B) | 11847 | 2-Chloroacetic acid; Chloroacetic Acid | 79-11-8 | C2H3ClO2 | 详情 | 详情 |
| (I) | 17527 | 2,6-Xylidine; 2,6-Dimethylaniline; 2,6-Dimethylphenylamine | 87-62-7 | C8H11N | 详情 | 详情 |
| (II) | 11296 | 2-Chloroacetyl chloride; Chloroacetic chloride | 79-04-9 | C2H2Cl2O | 详情 | 详情 |
| (III) | 24100 | 2-chloro-N-(2,6-dimethylphenyl)acetamide | 2198-53-0 | C10H12ClNO | 详情 | 详情 |
| (IV) | 39492 | 2-[(carboxymethyl)amino]acetic acid | 142-73-4 | C4H7NO4 | 详情 | 详情 |
| (V) | 39493 | 2-amino-N-(2,6-dimethylphenyl)acetamide | C10H14N2O | 详情 | 详情 |
Extended Information