N-Boc-4-哌啶甲醇合成路线 (共 71 条)
反应条件
[bis(2-methoxyethyl)amino]-sulfur trifluoride in tetrahydrofuran; dichloromethane T=0 - 20°C; 17 h;
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: EP1785418 A1, 2007 ;
Location in patent: Page/Page column 45 ;
反应条件
triphenylphosphine; diethylazodicarboxylate in dichloromethane T=20°C; 0.5 h;
参考文献
AstraZeneca AB
Patent: EP1244647 B1, 2006 ;
Location in patent: Page/Page column 22-23 ;
EP 1244647 B1
反应条件
1: 100 percent / ClCOCOCl; DMSO; Et3N / CH2Cl2 2: NaCNBH3; CF3CH2OH; 3A sieves 3: 100 percent / CF3COOH / CH2Cl2 View Scheme
参考文献
Ting, Pauline C; Lee, Joe F; Anthes, John C; Shih, Neng-Yang; Piwinski, John J
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 491 - 494
反应条件
1: oxalyl dichloride / dichloromethane; dimethyl sulfoxide / 0.25 h / -60 °C / Inert atmosphere 2: tetrahydrofuran / 20 °C 3: palladium 10 on activated carbon; hydrogen / methanol View Scheme
参考文献
Rossi, Cristina; Porcelloni, Marina; D'Andrea, Piero; Fincham, Christopher I.; Ettorre, Alessandro; Mauro, Sandro; Squarcia, Antonella; Bigioni, Mario; Parlani, Massimo; Nardelli, Federica; Binaschi, Monica; Maggi, Carlo A.; Fattori, Daniela
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2305 - 2308
反应条件
1: oxalyl dichloride / dichloromethane; dimethyl sulfoxide / 0.25 h / -60 °C / Inert atmosphere 2: tetrahydrofuran / 20 °C 3: palladium 10 on activated carbon; hydrogen / methanol 4: hydrogenchloride / 1,4-dioxane View Scheme
参考文献
Rossi, Cristina; Porcelloni, Marina; D'Andrea, Piero; Fincham, Christopher I.; Ettorre, Alessandro; Mauro, Sandro; Squarcia, Antonella; Bigioni, Mario; Parlani, Massimo; Nardelli, Federica; Binaschi, Monica; Maggi, Carlo A.; Fattori, Daniela
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2305 - 2308
反应条件
1: Dess-Martin periodane / dichloromethane 2: N-benzyl-trimethylammonium hydroxide / water; 1,4-dioxane 3: hydrogen; palladium on activated charcoal; hydrogenchloride / ethanol View Scheme
参考文献
MERCK SHARP and DOHME CORP.; DING, Fa-Xiang; DONG, Shuzhi; FRIE, Jessica; GU, Xin; JIANG, Jinlong; PASTERNAK, Alexander; TANG, Haifeng; WU, Zhicai; YU, Yang; SUZUKI, Takao
Patent: WO2014/15495 A1, 2014 ;
反应条件
pyridine; iodine; triphenylphosphine in benzene 1.5 h; Heating;
参考文献
Villalobos; Blake; Biggers; Butler; Chapin; Chen; Ives; Jones; Liston; Nagel; Nason; Nielsen; Shalaby; White
Journal of Medicinal Chemistry, 1994 , vol. 37, # 17 p. 2721 - 2734
反应条件
sodium iodide; triethanolamine in dichloromethane; acetone
参考文献
Merck and Co., Inc.
Patent: US6265434 B1, 2001 ;
US 6265434 B1
反应条件
1: 100 percent / ClCOCOCl; DMSO; Et3N / CH2Cl2 2: NaCNBH3; CF3CH2OH; 3A sieves View Scheme
参考文献
Ting, Pauline C; Lee, Joe F; Anthes, John C; Shih, Neng-Yang; Piwinski, John J
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 491 - 494
反应条件
1: 100 percent / ClCOCOCl; DMSO; Et3N / CH2Cl2 2: NaCNBH3; CF3CH2OH; 3A sieves View Scheme
参考文献
Ting, Pauline C; Lee, Joe F; Anthes, John C; Shih, Neng-Yang; Piwinski, John J
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 491 - 494