119285-07-3

基本信息
帕博西尼雜質(zhì)103
帕博西尼雜質(zhì)SMA-8
4-(5-氨基吡啶-2-基)哌嗪-1-羧酸叔丁酯
4-(5-氨基吡啶-2-YL)哌嗪-1-羧酸叔丁酯
Palbociclib Impurity 103
1-Boc-4-(5-amino-2-pyridinyl)-piperazine
1-BOC-4-(5-AMINO-PYRIDIN-2-YL)-PIPERAZINE
4-(5-Aminopyridin-2-yl)piperazine, N1-BOC protected
tert-butyl 3-allyl-3-hydroxyazetidine-43-carboxylate
4-(5-Aminopyridin-2-yl)piperazine, N1-BOC protected 95%
1-(tert-Butyloxycarbonyl)-4-(5-aminopyridin-2-yl)piperazine
4-(5-amino-2-pyridinyl)-2-piperazinecarboxylic acid tert-butyl ester
4-(5-AMINOPYRIDIN-2-YL)PIPERAZINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法

193902-78-2

119285-07-3
實(shí)施例197b 4-(5-氨基吡啶-2-基)哌嗪-1-羧酸叔丁酯197b的合成:在氮?dú)獗Wo(hù)下,向250-mL圓底燒瓶中加入1-叔丁基羰基-4-(5-硝基-2-哌啶)哌嗪197a(4.0g,13.0mmol)、10%鈀碳(濕潤(rùn),500mg)和甲醇(130mL)。將反應(yīng)體系抽真空后充入氫氣,于室溫下攪拌反應(yīng)15小時(shí)。反應(yīng)完成后,抽真空除去氫氣并充入氮?dú)狻7磻?yīng)混合物通過(guò)硅藻土墊過(guò)濾以去除催化劑,濾液經(jīng)減壓濃縮,得到目標(biāo)化合物197b(3.3g,收率91%)。質(zhì)譜數(shù)據(jù)(MS-ESI):[M + H]+ 279。
參考文獻(xiàn):
[1] Patent: US2005/182078, 2005, A1. Location in patent: Page/Page column 9; 12
[2] Patent: WO2007/53394, 2007, A1. Location in patent: Page/Page column 14
[3] Chinese Chemical Letters, 2013, vol. 24, # 4, p. 303 - 306
[4] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 16, p. 4779 - 4783
[5] Patent: EP2773638, 2015, B1. Location in patent: Paragraph 0753; 0755