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【结 构 式】 
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【分子编号】58811 【品名】[6-[(3-{[(allyloxy)carbonyl]amino}-5-methoxybenzyl)(tert-butoxycarbonyl)amino]-4-(4-morpholinyl)-2-pyridinyl]methyl methanesulfonate 【CA登记号】 |
【 分 子 式 】C28H38N4O9S 【 分 子 量 】606.69728 【元素组成】C 55.43% H 6.31% N 9.23% O 23.73% S 5.29% |
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：(XV)Amine (XII) was converted into allyl carbamate (XIII) by reaction with allyl chloroformate. The silylethoxymethyl protecting group of (XIII) was then removed by acidic treatment to provide alcohol (XIV), which was further activated as the corresponding mesylate (XV). Condensation of mesylate (XV) with 5-ethyl-2-mercaptothiazole (XVI) gave thioether (XVII). The N-Boc group of (XVII) was finally cleaved by treatment with trifluoroacetic acid to yield the title compound.
| 【1】 Fukami, T.; Mase, T.; Tsuchiya, Y.; Kanatani, A.; Fukuroda, T. (Banyu Pharmaceutical Co., Ltd.); Aminopyridine derivs.. EP 0889034; US 6011039; WO 9734873 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XII) | 58808 | tert-butyl 3-amino-5-methoxybenzyl[4-(4-morpholinyl)-6-({[2-(trimethylsilyl)ethoxy]methoxy}methyl)-2-pyridinyl]carbamate | C29H46N4O6Si | 详情 | 详情 | |
| (XIII) | 58809 | allyl 3-({(tert-butoxycarbonyl)[4-(4-morpholinyl)-6-({[2-(trimethylsilyl)ethoxy]methoxy}methyl)-2-pyridinyl]amino}methyl)-5-methoxyphenylcarbamate | C33H50N4O8Si | 详情 | 详情 | |
| (XIV) | 58810 | allyl 3-({(tert-butoxycarbonyl)[6-(hydroxymethyl)-4-(4-morpholinyl)-2-pyridinyl]amino}methyl)-5-methoxyphenylcarbamate | C27H36N4O7 | 详情 | 详情 | |
| (XV) | 58811 | [6-[(3-{[(allyloxy)carbonyl]amino}-5-methoxybenzyl)(tert-butoxycarbonyl)amino]-4-(4-morpholinyl)-2-pyridinyl]methyl methanesulfonate | C28H38N4O9S | 详情 | 详情 | |
| (XVI) | 58812 | 5-ethyl-1,3-thiazol-2-ylhydrosulfide; 5-ethyl-1,3-thiazole-2-thiol | C5H7NS2 | 详情 | 详情 | |
| (XVII) | 58813 | allyl 3-({(tert-butoxycarbonyl)[6-{[(5-ethyl-1,3-thiazol-2-yl)sulfanyl]methyl}-4-(4-morpholinyl)-2-pyridinyl]amino}methyl)-5-methoxyphenylcarbamate | C32H41N5O6S2 | 详情 | 详情 |
Extended Information