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【结 构 式】 
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【分子编号】43934 【品名】4-chloro[1,5]naphthyridine 【CA登记号】 |
【 分 子 式 】C8H5ClN2 【 分 子 量 】164.59388 【元素组成】C 58.38% H 3.06% Cl 21.54% N 17.02% |
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：(III)The known 4-hydroxy-1,5-naphthyridine-3-carboxylic acid (I) was decarboxylated to (II) upon refluxing in quinoline. Heating of (II) with POCl3 furnished 4-chloro-1,5-naphthyridine (III), which was converted to amine (IV) by reaction with n-propylamine in pyridine. Curtius rearrangement of 2-methyl-6-benzoxazolecarboxylic acid (V) in the presence of diphenylphosphoryl azide gave isocyanate (VI). Finally, coupling between isocyanate (VI) and amine (IV) provided the title urea.
| 【1】 Johns, A.; Porter, R.A. (SmithKline Beecham plc); Phenylurea and phenylthio urea derivs.. EP 1075478; WO 9958533 . |
| 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) | 43932 | 4-hydroxy[1,5]naphthyridine-3-carboxylic acid | C9H6N2O3 | 详情 | 详情 | |
| (II) | 43933 | [1,5]naphthyridin-4-ol | C8H6N2O | 详情 | 详情 | |
| (III) | 43934 | 4-chloro[1,5]naphthyridine | C8H5ClN2 | 详情 | 详情 | |
| (IV) | 43935 | [1,5]naphthyridin-4-amine; [1,5]naphthyridin-4-ylamine | C8H7N3 | 详情 | 详情 | |
| (V) | 43936 | 2-methyl-1,3-benzoxazole-6-carboxylic acid | C9H7NO3 | 详情 | 详情 | |
| (VI) | 43937 | 6-isocyanato-2-methyl-1,3-benzoxazole; 2-methyl-1,3-benzoxazol-6-yl isocyanate | C9H6N2O2 | 详情 | 详情 |
Extended Information