反-4-Boc-氨基环己醇合成路线 （共 13 条）
反应条件
1: trans-4-amino-cyclohexanol hydrochloride With sodium hydroxide in 1,4-dioxane; water T=0°C; 0.25 h; 2: di-tert-butyl dicarbonate in 1,4-dioxane; water T=20°C; 14 h;
参考文献
Carter, Percy H.; Cherney, Robert J.; Batt, Douglas G.; Brown, Gregory D.; Duncia, John V.; Gardner, Daniel S.; Yang, Michael G.
Patent: US2005/54626 A1, 2005 ;
Location in patent: Page/Page column 47 ;
US 20050054626 A1
反应条件
in acetonitrile T=20°C;
参考文献
Almirall, S.A.; Prat Quinones, Maria; Fonquerna Pou, Silvia; Puig Duran, Carlos; Lumeras Amador, Wenceslao; Aiguade Bosch, Jose; Caturla Javaloyes, Juan Francisco
Patent: EP2386555 A1, 2011 ;
Location in patent: Paragraph 0073 ;
反应条件
triethylamine in tetrahydrofuran
参考文献
Raju; Anandan, Sampathkumar; Gu, Shihai; Herradura, Prudencio; O'Dowd, Hardwin; Kim, Bum; Gomez, Marcela; Hackbarth, Corinne; Wu, Charlotte; Wang, Wen; Yuan, Zhengyu; White, Richard; Trias, Joaquim; Patel, Dinesh V.
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 12 p. 3103 - 3107
反应条件
1: trans-1-amino-4-cyclohexanol With thionyl chloride in chloroform Reflux; 2: di-tert-butyl dicarbonate With potassium carbonate; triethylamine in chloroform T=0 - 20°C; 11 h;
参考文献
Synthesis, , # 21 p. 3649 - 3653
反应条件
lithium aluminium tetrahydride in tetrahydrofuran Reflux;
参考文献
ALMIRALL, S.A.; AIGUADE BOSCH, Jose; GUAL ROIG, Silvia; PRAT QUINONES, Maria; PUIG DURAN, Carlos
Patent: WO2013/68552 A1, 2013 ;
Location in patent: Page/Page column 39 ;
反应条件
1: With triethylamine in dichloromethane T=0 - 20°C; 2.5 h; 2: With sodium hydrogencarbonate in dichloromethane; water 0.5 h;
参考文献
Xiong, Hui; Frietze, William; Andisik, Donald W.; Ernst, Glen E.; Palmer, William E.; Hinkley, Lindsay; Varnes, Jeffrey G.; Albert, Jeffrey S.; Veale, Chris A.
Tetrahedron Letters, 2010 , vol. 51, # 51 p. 6741 - 6744
反应条件
oxalyl dichloride; dimethyl sulfoxide; triethylamine in dichloromethane T=-78 - 20°C; 1.5 h;
参考文献
Noguchi, Hirohide; Aoyama, Toyohiko; Shioiri, Takayuki
Heterocycles, 2002 , vol. 58, p. 471 - 504
反应条件
1.1: triphenylphosphine / THF-d8 (tetrahydrofuran-d8) / 0.25 h / 20 °C / |Inert atmosphere 1.2: 18.03 h / 20 °C 2.1: sodium hydroxide / tetrahydrofuran / 18 h / 85 °C View Scheme
参考文献
IMPERIAL INNOVATIONS LIMITED; LEATHERBARROW, Robin; TATE, Edward; YU, Zhiyong; RACKHAM, Mark
Patent: WO2013/83991 A1, 2013 ;
反应条件
1.1: triethylamine / tetrahydrofuran / 0 °C / Inert atmosphere 1.2: 3 h / 0 - 5 °C 2.1: dichloromethane / 20 °C / Inert atmosphere 3.1: sodium hydroxide; water / dichloromethane / 25 °C 3.2: 0.5 h View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; ZHANG, Beili; KRAWIEC, Mariusz; LUISI, Brian; MEDEK, Ales
Patent: WO2011/50220 A1, 2011 ;
WO 2011/050220 A1
反应条件
1: With triethylamine in dichloromethane
T=0°C; 0.833333 h; Inert atmosphere;
2: With potassium tert-butylate in tetrahydrofuran
T=20°C; 16 h; Inert atmosphere;
参考文献
Harty, Matthew; Nagar, Mitesh; Atkinson, Logan; Legay, Christina M.; Derksen, Darren J.; Bearne, Stephen L.
Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 1 p. 390 - 393
