733039-20-8

基本信息
帕布西利布中間體
LEE011中間體1
2-氯-4-環(huán)戊胺基-5-溴嘧啶
2-氯-4-環(huán)戊氨基-5-溴嘧啶
5-溴-2-氯-N-環(huán)戊胺嘧啶-4胺
5-溴-2-氯-N-環(huán)戊胺嘧啶-4胺
2-氯-5-溴-N-環(huán)戊基-4-嘧啶胺
5-溴-2-氯-N-環(huán)戊烷嘧啶-4-氨
5-溴-2-氯-4-(環(huán)戊基氨基)嘧啶
5-Bromo-2-chloro-N-cyclopentyl-4-pyrimidinamine
5-Bromo-2-chloro-4-(cyclopentylamino)pyrimidine
5-broMo-2-chloro-N-cyclopentylpyriMidin-4-aMine
4-PyriMidinaMine, 5-broMo-2-chloro-N-cyclopentyl-
(5-Bromo-2-chloro-pyrimidin-4-yl)-cyclopentyl-amine
N-(5-Bromo-2-chloropyrimidin-4-yl)(cyclopentyl)amine
5-broMo-2-chloro-N-cyclopentylpyriMidin-4-aMine ISO 9001:2015 REACH
物理化學(xué)性質(zhì)
制備方法

36082-50-5

1003-03-8

733039-20-8
在室溫條件下,將5-溴-2,4-二氯嘧啶(45.6 g,200 mmol)溶解于二惡烷(400 mL)中,隨后向該溶液中加入環(huán)戊胺(20.4 g,240 mmol)。將反應(yīng)混合物在室溫下持續(xù)攪拌6小時。反應(yīng)完成后,用乙酸乙酯稀釋反應(yīng)混合物,依次用飽和食鹽水洗滌,并經(jīng)無水硫酸鎂干燥。減壓濃縮除去溶劑,得到5-溴-2-氯-N-環(huán)戊基-4-嘧啶胺,為淺黃色固體(56 g,產(chǎn)率100%),該產(chǎn)物無需進一步純化即可用于后續(xù)反應(yīng)。產(chǎn)物表征數(shù)據(jù)如下:1H NMR (500 MHz, DMSO-d6) δ 8.23 (1H, s), 7.37 (1H, d, J = 7.3 Hz), 4.31 (1H, m), 1.92 (2H, m), 1.71 (2H, m), 1.53-1.59 (4H, m) ppm; LCMS-ESI (POS), m/z [M + H]+: 實測值 276.0, 計算值 275.9。
參考文獻:
[1] Patent: WO2009/85185, 2009, A1. Location in patent: Page/Page column 35
[2] Journal of Medicinal Chemistry, 2014, vol. 57, # 8, p. 3430 - 3449
[3] Combinatorial Chemistry and High Throughput Screening, 2017, vol. 20, # 8, p. 703 - 712
[4] Patent: WO2010/20675, 2010, A1. Location in patent: Page/Page column 89
[5] Patent: US2012/115878, 2012, A1. Location in patent: Page/Page column 5-6