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【结 构 式】 
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【药物名称】Ponalrestat, MK-538, ICI-128436, Prodiax, Statil 【化学名称】3-(4-Bromo-2-fluorobenzyl)-4-oxo-3,4-dihydro-1-phthalazineacetic acid 【CA登记号】72702-95-5, 72703-73-2 (Na salt) 【 分 子 式 】C17H12BrFN2O3 【 分 子 量 】391.19919 |
【开发单位】AstraZeneca (Originator), Banyu (Licensee) 【药理作用】ENDOCRINE DRUGS, METABOLIC DRUGS, Symptomatic Antidiabetic Agents, Treatment of Diabetic Complications, Treatment of Disorders of Purine and Pyrimidine Metabolism, Treatment of Gout, Uricosurics, Aldose Reductase Inhibitors |
合成路线1
The condensation of ethyl 3,4-dihydro-4-oxo-phthalazine-1-acetate (I) with 4-bromo-2-fluoro benzyl bromide (II) by means of NaH in hot DMF gives ethyl 3-(4-bromo-2-fluorobenzyl)-3,4-dihydro-4-oxophthalazine-1-acetate (III), which is saponified with KOH in refluxing ethanol.
| 【1】 Pfaffli, P. (Novartis AG); Increasing vigilance or treating cerebral insuffi. GB 1492579; US 4146643 . |
| 【2】 Castaner, J.; Prous, J.; ICI-128436. Drugs Fut 1987, 12, 4, 347. |
| 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) | 12095 | ethyl 2-(4-oxo-3,4-dihydro-1-phthalazinyl)acetate; Ethyl 3,4-dihydro-4-oxo-1-phthalazineacetate | 25947-13-1 | C12H12N2O3 | 详情 | 详情 |
| (II) | 22904 | 2-fluoro-4-bromobenzyl bromide; 4-bromo-1-(bromomethyl)-2-fluorobenzene | 76283-09-5 | C7H5Br2F | 详情 | 详情 |
| (III) | 22905 | ethyl 2-[3-(4-bromo-2-fluorobenzyl)-4-oxo-3,4-dihydro-1-phthalazinyl]acetate | C19H16BrFN2O3 | 详情 | 详情 |