4-N-Boc-氨基环己酮合成路线 （共 23 条）
反应条件
1: 93 percent / aq. NaOH / dioxane / 2 h / 20 °C 2: 98 percent / (COCl)2; Me2SO; Et3N / CH2Cl2 / 1.5 h / -78 - 20 °C View Scheme
参考文献
Heterocycles, , vol. 58, p. 471 - 504
反应条件
bromine; AlCl3, aluminium chloride in ethyl acetate T=0°C; 0.25 h;
参考文献
GLAXO GROUP LIMITED
Patent: WO2008/128961 A1, 2008 ;
Location in patent: Page/Page column 31; 52 ;
WO 2008/128961 A1
反应条件
diethylamino-sulfur trifluoride in dichloromethane T=20°C; Inert atmosphere;
参考文献
WO2010/111406 A2, ;
Page/Page column 104 ;
WO 2010/111406 A2
反应条件
1: phenyl-carbamic acid tert-butyl ester With tert.-butyl lithium in tetrahydrofuran; pentane T=-70 - -20°C; 2.5 h; 2: (4-oxo-cyclohexyl)-carbamic acid tert-butyl ester With potassium tert-butylate in tetrahydrofuran; pentane T=-70 - 20°C; 3: With hydrogenchloride in tetrahydrofuran; diethyl ether; water; pentane T=0°C; pH=7;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2008/21375 A2, 2008 ;
Location in patent: Page/Page column 42-43 ;
WO 2008/021375 A2
反应条件
1: 100 percent / DMAP / tetrahydrofuran / 2 h / Heating
2: (R,R)-bis(α-methylbenzyl)amine hydrochloride; BuLi / tetrahydrofuran; dimethylformamide; hexane / 4 h / -45 °C
3: 83 percent / NaBH4 / methanol / 2.5 h / -98 - -60 °C
4: Et3N / CH2Cl2 / 4 h / 20 °C
5: TFA / CH2Cl2 / 15 h / 20 °C
6: 26.5 mg / CHCl3 / 60 h / Heating
View Scheme
参考文献
Aggarwal, Varinder K.; Olofsson, Berit
Angewandte Chemie - International Edition, 2005 , vol. 44, # 34 p. 5516 - 5519
反应条件
potassium tert-butylate in tetrahydrofuran; hexane; water
参考文献
KBP Biosciences Co., Ltd.; ZHANG, Hui; DONG, Yanyan
Patent: EP2738156 A1, 2014 ;
Location in patent: Page/Page column ;
反应条件
1: triphenyl-methyl-phosphonium iodide With potassium tert-butylate in tetrahydrofuran
T=20°C; 3 h;
2: (4-oxo-cyclohexyl)-carbamic acid tert-butyl ester in tetrahydrofuran
T=0 - 20°C; 10 h;
参考文献
RANBAXY LABORATORIES LIMITED
Patent: WO2005/21515 A2, 2005 ;
Location in patent: Page/Page column 73 ;
WO 2005/021515 A2
反应条件
diethylamino-sulfur trifluoride in dichloromethane
15 h;
参考文献
GLAXO GROUP LIMITED
Patent: WO2004/50619 A1, 2004 ;
Location in patent: Page 71 ;
WO 2004/050619 A1
反应条件
diethylamino-sulfur trifluoride in dichloromethane
T=-5 - 20°C; Inert atmosphere;
参考文献
AGIOS PHARMACEUTICALS, INC.; LEMIEUX, Rene M.; POPOVICI-MULLER, Janeta; TRAVINS, Jeremy; CAI, Zhenwei; CUI, Dawei; ZHOU, Ding
Patent: WO2013/107291 A1, 2013 ;
Location in patent: Page/Page column 64 ;
反应条件
sodium tetrahydroborate; diethylamino-sulfur trifluoride; 3-chloro-benzenecarboperoxoic acid in methanol; water; ethyl acetate; Petroleum ether
参考文献
AGIOS PHARMACEUTICALS, INC; Lemieux, Rene M.; Popovici-Muller, Janeta; Travins, Jeremy; Cai, Zhenwei; Cui, Dawei; Zhou, Ding
Patent: US2013/190249 A1, 2013 ;
Location in patent: Page/Page column ;
