N-Boc-4-哌啶甲醇合成路线 （共 71 条）
反应条件
methanesulfonyl chloride; triethylamine in tetrahydrofuran T=0°C; 1 h;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2004/58781 A1, 2004 ;
Location in patent: Page 102-103 ;
WO 2004/058781 A1
反应条件
triethanolamine in dichloromethane
参考文献
Amgen Inc.
Patent: US6878714 B2, 2005 ;
US 6878714 B2
反应条件
4-(N,N-dimethlyamino)pyridine; triethylamine in CH2Cl2.; dichloromethane; water
参考文献
Chee, Jennifer; Johanson, Jill N.; Kayser, Frank; Parsons, William H.; Rupprecht, Kathleen M.
Patent: US2002/13348 A1, 2002 ;
反应条件
1: 69 percent / triphenylphosphine; diisopropyl azodicarboxylate / tetrahydrofuran / 72 h / 20 °C
2: trifluoroacetic acid
View Scheme
参考文献
Waterhouse; Collier; O'Brien
Journal of Labelled Compounds and Radiopharmaceuticals, 1996 , vol. 38, # 3 p. 215 - 226
反应条件
1: 92 percent / triphenylphosphine; diethyl azodicarboxylate / CH2Cl2; toluene / 1 h / 20 °C
2: HCl / dioxane / 1 h / 20 °C
3: 80 percent / formic acid / H2O / 95 °C
4: nitric acid; trifluoroacetic acid / CH2Cl2 / 20 °C
5: hydrogen / palladium on activated carbon / methanol
6: 2-methoxy-ethanol / 2 h / 115 °C
View Scheme
参考文献
Hennequin, Laurent F.; Stokes, Elaine S. E.; Thomas, Andrew P.; Johnstone, Craig; Ple, Patrick A.; Ogilvie, Donald J.; Dukes, Michael; Wedge, Stephen R.; Kendrew, Jane; Curwen, Jon O.
Journal of Medicinal Chemistry, 2002 , vol. 45, # 6 p. 1300 - 1312
反应条件
1: pyridine / CH2Cl2
2: HCl / ethyl acetate
View Scheme
参考文献
Kikuchi, Tatsuya; Zhang, Ming-Rong; Ikota, Nobuo; Fukushi, Kiyoshi; Okamura, Toshimitsu; Suzuki, Kazutoshi; Arano, Yasushi; Irie, Toshiaki
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 8 p. 1927 - 1930
反应条件
triphenylphosphine; diethylazodicarboxylate in dichloromethane; toluene
T=20°C; 1 h;
参考文献
Seimbille, Yann; Phelps, Michael E.; Czernin, Johannes; Silverman, Daniel H. S.
Journal of Labelled Compounds and Radiopharmaceuticals, 2005 , vol. 48, # 11 p. 829 - 843
反应条件
1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 1.33 h / 0 - 20 °C
2.1: sodium hydride / N,N-dimethyl-formamide; mineral oil / 0.25 h / 20 °C / Inert atmosphere
2.2: 16 h / 50 °C
3.1: hydrogenchloride / 1,4-dioxane / 3 h / 20 °C
View Scheme
参考文献
MERCK SHARP and DOHME CORP.; TING, Pauline, C.; ASLANIAN, Robert; CAO, Jianhua; KIM, David; ZORN, Nicolas
Patent: WO2012/24179 A1, 2012 ;
反应条件
1: 70 percent / PCC / CH2Cl2 / 20 °C
2: 61 percent / NaH / dimethylsulfoxide / 20 °C
View Scheme
参考文献
Someya, Hidenori; Kondoh, Azusa; Sato, Akinori; Ohmiya, Hirohisa; Yorimitsu, Hideki; Oshima, Koichiro
Synlett, 2006 , # 18 p. 3061 - 3064
反应条件
1: triphenylphosphine; diethylazodicarboxylate / tetrahydrofuran / 0 - 20 °C / Inert atmosphere
2: hydrogenchloride / dichloromethane; 1,4-dioxane / 20 °C / Cooling
View Scheme
参考文献
FAB PHARMA SAS; GERUSZ, Vincent; ESCAICH, Sonia; OXOBY, Mayalen; DENIS, Alexis
Patent: WO2011/61214 A1, 2011 ;
WO 2011/061214 A1
