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【结 构 式】 
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【分子编号】12408 【品名】6-Amino-2-pyridinol 【CA登记号】 |
【 分 子 式 】C5H6N2O 【 分 子 量 】110.11552 【元素组成】C 54.54% H 5.49% N 25.44% O 14.53% |
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：(II)The hydrolysis of 2,6-diaminopyridine (I) in 36% aqueous hydrochloric acid leads to 2-amino-6-hydroxypyridine (II), which can be converted by several ways to the final product CGP 28014. Two are described here: a) Conversion of 2-amino-6-hydroxypyridine (II) with N,N-dimethylformamide diethylacetal gives the N-(2-oxopyridin-6-yl)-N',N'-dimethylformamidine (IV), which is transaminated with dipropylamine to CGP 28014. b) Reaction of 2-amino-6-hydroxypyridine (II) with ethyl-N-cyanoformimidate (2) yields N-(2-oxopyridin-6-yl)-N'-cyanoformamidine (III), which is heated with dipropylamine to give CGP 28014.
| 【1】 Donetti, A.; Bellora, E.; Cereda, E.; A new convenient synthesis of H2-aryl-H1-alkylformamidines and N2-aryl-N1,N1-dialkylformamidines. Synthesis 1986, 288-91. |
| 【2】 Von Sprecher, G.; Waldmeier, P. (Novartis AG); Pyridine derivs. EP 0239533; JP 1987226959; US 4683938 . |
| 【3】 Mobius, H.J.; Waldmeier, P.C.; Von Sprecher, G.; CGP 28014. Drugs Fut 1992, 17, 4, 275. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 24747 | ethyl cyanoiminoformate | C4H6N2O | 详情 | 详情 | ||
| (I) | 12407 | 2,6-Pyridinediamine; 6-Amino-2-pyridinylamine; 2,6-Diaminopyridine | 141-86-6 | C5H7N3 | 详情 | 详情 |
| (II) | 12408 | 6-Amino-2-pyridinol | C5H6N2O | 详情 | 详情 | |
| (III) | 12409 | N'-Cyano-N-(6-oxo-1,6-dihydro-2-pyridinyl)iminoformamide | C7H6N4O | 详情 | 详情 | |
| (IV) | 12410 | N,N-Dimethyl-N'-(6-oxo-1,6-dihydro-2-pyridinyl)iminoformamide | C8H11N3O | 详情 | 详情 |
Extended Information