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【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