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【结 构 式】 
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【药物名称】Florfenicol, Sch-25298 【化学名称】2,2-Dichloro-N-[(1S,2R)-1-(fluoromethyl)-2-hydroxy-2-[4-(methylsulfonyl)phenyl]ethyl]acetamide 【CA登记号】76639-94-6 【 分 子 式 】C12H14Cl2FNO4S 【 分 子 量 】358.21808 |
【开发单位】Schering-Plough 【药理作用】Antibacterial Drugs, ANTIINFECTIVE THERAPY |
合成路线1
The D-(threo)-1-p-substituted-phenyl-2-dichloroacetamido-3-fluoro-1-propanol derivatives were prepared according to the following reaction sequence: The amino group of (I) was protected with phthalicanhydride (II), followed by substitution of the primary hydroxy group with diethylamine - sulfur-trifluoride to (III), deprotection with hydrazine to the amine (IV) and acetylation with methyldichloro-acetate (B) to the target compounds.
| 【1】 Kwung-ping Fu; SCH-24893 and SCH-25298. Drugs Fut 1982, 7, 3, 172. |
| 【2】 Nagabhushan, T.L.; et al.; EP 0800820 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (A) | 11900 | 2-Benzofuran-1,3-dione;1,2-Benzenedicarboxylic Anhydride;1,2-BENZENE DICARBOXYLIC ACID ANHYDRIDE;1,2-BENZENEDICARBONIC ACID, ANHYDRIDE;1,3-DIOXOPHTHALAN;1,3-ISOBENZOFURANDIONE;o-phthalic anhydride; Phthalic anhydride | 85-44-9 | C8H4O3 | 详情 | 详情 |
| (B) | 36413 | methyl 2,2-dichloroacetate | 116-54-1 | C3H4Cl2O2 | 详情 | 详情 |
| (I) | 36409 | (1R,2R)-2-amino-1-[4-(methylsulfonyl)phenyl]-1,3-propanediol | 51458-28-7 | C10H15NO4S | 详情 | 详情 |
| (II) | 36410 | 2-[(1R,2R)-2-hydroxy-1-(hydroxymethyl)-2-[4-(methylsulfonyl)phenyl]ethyl]-1H-isoindole-1,3(2H)-dione | C18H17NO6S | 详情 | 详情 | |
| (III) | 36411 | 2-[(1S,2R)-1-(fluoromethyl)-2-hydroxy-2-[4-(methylsulfonyl)phenyl]ethyl]-1H-isoindole-1,3(2H)-dione | C18H16FNO5S | 详情 | 详情 | |
| (IV) | 36412 | (1R,2S)-2-amino-3-fluoro-1-[4-(methylsulfonyl)phenyl]-1-propanol | C10H14FNO3S | 详情 | 详情 |
Extended Information