【结 构 式】 |
【分子编号】58379 【品名】N-(4-aminophenyl)-N-methylacetamide; 4'-amino-N-methylacetanilide 【CA登记号】 |
【 分 子 式 】C9H12N2O 【 分 子 量 】164.20716 【元素组成】C 65.83% H 7.37% N 17.06% O 9.74% |
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:(IV)2,6-Dichloropurine (I) is condensed with cyclobutylamine (II) in the presence of diisopropylethylamine in hot butanol to produce the 6-cyclobutylamino purine (III). The 2-chloro group of purine (III) is then displaced with 4-amino-N-methylacetanilide (IV) in N-methylpyrrolidone at 145 C to furnish the target diamino purine derivative.
【1】 Bammerlin, H.; Le Grand, D.; Hayler, J.; et al.; Novel 2,6-disubstituted purines - The synthesis of potent and selective inhibitors of the protein tyrosine kinase Syk. Drugs Fut 2002, 27, Suppl. A. |
【2】 Menear, K.A.; Mattes, H.; Collingwood, S.P.; Walker, C.V.; Hayler, J.; Le Grand, D.M.; Cockcroft, X.-L. (Novartis AG; Novartis-Erfindungen VmbH); Purine derivs. inhibitors of tyrosine protein kinase syk. EP 1200435; WO 0109134 . |
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) | 25254 | 2,6-dichloro-9H-purine | 5451-40-1 | C5H2Cl2N4 | 详情 | 详情 |
(II) | 58377 | cyclobutylamine; cyclobutanamine; Aminocyclobutane | 2516-34-9 | C4H9N | 详情 | 详情 |
(III) | 58378 | 2-chloro-N-cyclobutyl-9H-purin-6-amine; N-(2-chloro-9H-purin-6-yl)-N-cyclobutylamine | C9H10ClN5 | 详情 | 详情 | |
(IV) | 58379 | N-(4-aminophenyl)-N-methylacetamide; 4'-amino-N-methylacetanilide | C9H12N2O | 详情 | 详情 |
Extended Information