1005-37-4

基本信息
6-氯-N'-甲基嘧啶-2,4-二胺
6-氯-N'-甲基-嘧啶-2,4-二胺
6-氯-N~4~-甲基-2,4-嘧啶二胺
(2-氨基-6-氯-嘧啶-4-基)-甲基-胺
Methyl-2,4-pyriMidinediaMine
2-amino-4-methylamino-6-chloropyrimidine
6-chloro-N'-methylpyrimidine-2,4-diamine
6-chloro-N'-methyl-pyrimidine-2,4-diamine
(2-amino-6-chloro-pyrimidin-4-yl)-methyl-amine
6-Chloro-N4-methylpyrimidine-2,4-diaminevfc'b'g
6-chloro-N~4~-methyl-2,4-pyrimidinediamine(SALTDATA: FREE)
制備方法

56-05-3

74-89-5

1005-37-4
以2-氨基-4,6-二氯嘧啶和甲胺為原料合成6-氯-N4-甲基嘧啶-2,4-二胺的一般步驟如下:首先,將4,6-二氯嘧啶-2-胺(3.28g,20.0mmol)、甲胺(12.0mL,24.0mmol,作為2M甲醇溶液)和Hunig堿在正丁醇(20mL)中的混合物加熱至50℃,然后升溫至95℃反應(yīng)過(guò)夜。反應(yīng)完成后,將混合物濃縮,粗產(chǎn)物溶于乙酸乙酯(300mL)中,并用水(3×150mL)洗滌。有機(jī)層用硫酸鎂干燥,過(guò)濾后濃縮,得到淺黃色固體的目標(biāo)產(chǎn)物6-氯-N4-甲基嘧啶-2,4-二胺(2.90g,收率91%)。LCMS分析顯示[M + H]+峰為159。
參考文獻(xiàn):
[1] Patent: WO2015/187089, 2015, A1. Location in patent: Page/Page column 70
[2] Patent: CN108191774, 2018, A. Location in patent: Paragraph 0203; 0204; 0205
[3] Patent: US6677345, 2004, B1. Location in patent: Page/Page column 12
[4] Patent: WO2010/120854, 2010, A1. Location in patent: Page/Page column 87
[5] Journal of Medicinal Chemistry, 2011, vol. 54, # 6, p. 1871 - 1895