1-Boc-3-羟基哌啶合成路线 （共 34 条）
反应条件
sodium hydroxide in methanol T=20°C; 2 h;
参考文献
Journal of Labelled Compounds and Radiopharmaceuticals, , vol. 44, # 1 p. 31 - 41
反应条件
1: 96 percent / Et3N / tetrahydrofuran / 1 h / Ambient temperature 2: 98 percent / NaN3 / dimethylformamide / 48 h / 70 °C 3: 69 percent / H2 / 10percent Pd/C / acetic acid; methanol / 24 h / 2585.7 Torr / Ambient temperature View Scheme
参考文献
Kovackova, Sona; Dracinsky, Martin; Rejman, Dominik
Tetrahedron, 2011 , vol. 67, # 7 p. 1485 - 1500
反应条件
triethylamine in dichloromethane T=0 - 20°C; 3 h;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; Charrier, Jean-Damien; Durrant, Steven John; Knegtel, Ronald
Patent: US2013/115310 A1, 2013 ;
Location in patent: Paragraph 0248; 0249 ;
反应条件
4-(N,N-dimethlyamino)pyridine; triethylamine in tetrahydrofuran T=20°C; 16 h;
参考文献
BIOGEN IDEC MA INC.; SUNESIS PHARMACEUTICALS, INC.; HOPKINS, Brian, T.; SCOTT, Daniel; CONLON, Patrick; JENKINS, Tracy, J.; POWELL, Noel; GUAN, Bing; CURERVO, Julio, H.; WANG, Deping; TAVERAS, Art
Patent: WO2012/58645 A1, 2012 ;
Location in patent: Page/Page column 210 ;
WO 2012/058645 A1
反应条件
in tetrahydrofuran; ethyl acetate
参考文献
The United States of America as represented by the Department of Health and Human Services
Patent: US5571832 A1, 1996 ;
US 5571832 A
反应条件
1.1: 89 percent / NaH / tetrahydrofuran / 6 h / 20 °C 2.1: s-BuLi; TMEDA / tetrahydrofuran; cyclohexane / 5 h / -78 °C 2.2: 80 percent / tetrahydrofuran; cyclohexane / 0.08 h / -78 °C 3.1: 87 percent / H2 / (S)-BINAP; RuCl2 / methanol / 11 h / 45 °C / 51716.2 Torr 4.1: 97 percent / BH3*THF / tetrahydrofuran / 3 h / 20 °C 5.1: 98 percent / oxalyl chloride; DMSO; DIPEA / CH2Cl2 / -78 - 20 °C View Scheme
参考文献
Wilkinson; Stehle; Beak
Organic letters, 2000 , vol. 2, # 2 p. 155 - 158
反应条件
1.1: 89 percent / NaH / tetrahydrofuran / 6 h / 20 °C 2.1: s-BuLi; TMEDA / tetrahydrofuran; cyclohexane / 5 h / -78 °C 2.2: 80 percent / tetrahydrofuran; cyclohexane / 0.08 h / -78 °C 3.1: 87 percent / H2 / (S)-BINAP; RuCl2 / methanol / 11 h / 45 °C / 51716.2 Torr View Scheme
参考文献
Wilkinson; Stehle; Beak
Organic letters, 2000 , vol. 2, # 2 p. 155 - 158
反应条件
1: tert-butyl 3-hydroxy-1-piperidinecarboxylate With 2,2,6,6-tetramethyl-piperidine-N-oxyl; [bis(acetoxy)iodo]benzene in dichloromethane 16 h; 2: benzylamine With sodium tris(acetoxy)borohydride in dichloromethane chemoselective reaction;
参考文献
Guerin, Claire; Bellosta, Veronique; Guillamot, Gerard; Cossy, Janine
Organic Letters, 2011 , vol. 13, # 13 p. 3534 - 3537
反应条件
1.1: 89 percent / NaH / tetrahydrofuran / 6 h / 20 °C
2.1: s-BuLi; TMEDA / tetrahydrofuran; cyclohexane / 5 h / -78 °C
2.2: 80 percent / tetrahydrofuran; cyclohexane / 0.08 h / -78 °C
3.1: 87 percent / H2 / (S)-BINAP; RuCl2 / methanol / 11 h / 45 °C / 51716.2 Torr
4.1: 97 percent / BH3*THF / tetrahydrofuran / 3 h / 20 °C
5.1: 98 percent / oxalyl chloride; DMSO; DIPEA / CH2Cl2 / -78 - 20 °C
6.1: 79 percent / n-BuLi / tetrahydrofuran; hexane / -78 - 20 °C
7.1: 94 percent / H2 / Pd/C / ethyl acetate / 24 h
View Scheme
参考文献
Wilkinson; Stehle; Beak
Organic letters, 2000 , vol. 2, # 2 p. 155 - 158
反应条件
1: 90 percent / NaH / toluene / 0.25 h / 75 °C
2: 87 percent / CF3CO2H / 2 h
View Scheme
参考文献
Wang, Xueqing; Bhatia, Pramila A.; Daanen, Jerome F.; Latsaw, Steve P.; Rohde, Jeffrey; Kolasa, Teodozyi; Hakeem, Ahmed A.; Matulenko, Mark A.; Nakane, Masaki; Uchic, Marie E.; Miller, Loan N.; Chang, Renjie; Moreland, Robert B.; Brioni, Jorge D.; Stewart, Andrew O.
Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 15 p. 4667 - 4678
