2-(4-氨基苯)-1,1,1,3,3,3-六氟-2-丙醇合成路线 （共 6 条）
反应条件
toluene-4-sulfonic acid T=130°C; 14 h;
参考文献
Li, Leping; Liu, Jiwen; Zhu, Liusheng; Cutler, Serena; Hasegawa, Hirohiko; Shan, Bei; Medina, Julio C.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 6 p. 1638 - 1642
反应条件
2,6-dimethylpyridine in acetone T=80°C; 24 h; Inert atmosphere; Product distribution / selectivity;
参考文献
GRIFFIN, Patrick R.; ROUSH, William R.; KUMAR, Naresh; NUHANT, Philippe; BURRIS, Thomas; SOLT, Laura
Patent: WO2011/115892 A1, 2011 ;
Location in patent: Page/Page column 6; 45; 46 ;
WO 2011/115892 A1
反应条件
2,6-dimethylpyridine in acetone T=60°C; 18 h; Inert atmosphere;
参考文献
Solt, Laura A.; Kumar, Naresh; Nuhant, Philippe; Wang, Yongjun; Lauer, Janelle L.; Liu, Jin; Istrate, Monica A.; Kamenecka, Theodore M.; Roush, William R.; Vidovic, Dusica; Schuerer, Stephan C.; Xu, Jihong; Wagoner, Gail; Drew, Paul D.; Griffin, Patrick R.; Burris, Thomas P.
Nature, 2011 , vol. 472, # 7344 p. 491 - 494
反应条件
N-ethyl-N,N-diisopropylamine in dichloromethane T=20°C; 8 h; Inert atmosphere;
参考文献
GRIFFIN, Patrick R.; ROUSH, William R.; KUMAR, Naresh; NUHANT, Philippe; BURRIS, Thomas; SOLT, Laura
Patent: WO2011/115892 A1, 2011 ;
Location in patent: Page/Page column 5; 87; 88 ;
WO 2011/115892 A1
反应条件
1: With 4-(N,N-dimethlyamino)pyridine; triethylamine in dichloromethane
T=20°C; 22 h;
2: With lithium aluminium tetrahydride in tetrahydrofuran
T=0°C; 16 h;
参考文献
Orphagen Pharmaceuticals; Thacher, Scott; Li, Xiaolin; Babine, Robert; Tse, Bruno
Patent: US8389739 B1, 2013 ;
Location in patent: Page/Page column 30 ;
US 8389739 B1
反应条件
1.1: Py
1.2: aq. NaOH
2.1: 96 percent / BH3*THF
View Scheme
参考文献
Panday, Narendra; Benz, Joerg; Blum-Kaelin, Denise; Bourgeaux, Vanessa; Dehmlow, Henrietta; Hartman, Peter; Kuhn, Bernd; Ratni, Hassen; Warot, Xavier; Wright, Matthew B.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 19 p. 5231 - 5237
