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【结 构 式】 
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【分子编号】49147 【品名】N-[3-([5-methyl-2-[4-(trifluoromethoxy)phenyl]-1,3-oxazol-4-yl]methoxy)benzyl]hydroxylamine; 4-([3-[(hydroxyamino)methyl]phenoxy]methyl)-5-methyl-2-[4-(trifluoromethoxy)phenyl]-1,3-oxazole 【CA登记号】 |
【 分 子 式 】C19H17F3N2O4 【 分 子 量 】394.3502696 【元素组成】C 57.87% H 4.35% F 14.45% N 7.1% O 16.23% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(V)Condensation of the (chloromethyl)oxazole (I) with 3-hydroxybenzaldehyde (II) in the presence of K2CO3 afforded ether (III). The aldehyde group of (III) was then converted to oxime (IV) upon treatment with hydroxylamine hydrochloride and sodium acetate. Reduction of oxime (IV) with NaBH3CN produced the hydroxylamine (V). This was finally condensed with N-(chlorocarbonyl)isocyanate to produce the target oxadiazolidine dione.
| 【1】 Malamas, M.S.; et al.; Antihyperglycemic activity of new 1,2,4-oxadiazolidine-3,5-diones. Eur J Med Chem 2001, 36, 1, 31. |
| 【2】 Malamas, M.S.; Palka, C.L.; Gunawan, I. (American Home Products Corp.); Aralkyl-1,2,4-oxadiazolidine-3,5-diones as antihyperglycemic agents. US 5480896 . |
| 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) | 49144 | 4-(chloromethyl)-5-methyl-2-[4-(trifluoromethoxy)phenyl]-1,3-oxazole; 4-[4-(chloromethyl)-5-methyl-1,3-oxazol-2-yl]phenyl trifluoromethyl ether | C12H9ClF3NO2 | 详情 | 详情 | |
| (II) | 28537 | 3-hydroxybenzaldehyde | 100-83-4 | C7H6O2 | 详情 | 详情 |
| (III) | 49145 | 3-([5-methyl-2-[4-(trifluoromethoxy)phenyl]-1,3-oxazol-4-yl]methoxy)benzaldehyde | C19H14F3NO4 | 详情 | 详情 | |
| (IV) | 49146 | 3-([5-methyl-2-[4-(trifluoromethoxy)phenyl]-1,3-oxazol-4-yl]methoxy)benzaldehyde oxime | C19H15F3N2O4 | 详情 | 详情 | |
| (V) | 49147 | N-[3-([5-methyl-2-[4-(trifluoromethoxy)phenyl]-1,3-oxazol-4-yl]methoxy)benzyl]hydroxylamine; 4-([3-[(hydroxyamino)methyl]phenoxy]methyl)-5-methyl-2-[4-(trifluoromethoxy)phenyl]-1,3-oxazole | C19H17F3N2O4 | 详情 | 详情 |
Extended Information