2-氯-6-三氟甲基烟酸合成路线 （共 12 条）
反应条件
1: 2-chloro-6-trifluoromethyl pyridine With n-butyllithium; diisopropylamine in tetrahydrofuran; hexane T=-85°C; 4 h; 2: carbon dioxide in tetrahydrofuran; hexane 3: With hydrogenchloride in tetrahydrofuran; hexane T=25°C; Further stages.;
参考文献
Cottet, Fabrice; Schlosser, Manfred
European Journal of Organic Chemistry, 2004 , # 18 p. 3793 - 3798
反应条件
1: 2-chloro-6-trifluoromethyl pyridine With lithium chloride in tetrahydrofuran T=20°C; 1 h; 2: carbon dioxide in tetrahydrofuran
参考文献
INCYTE CORPORATION; RODGERS, James D.; SHEPARD, Stacey; ZHU, Wenyu; SHAO, Lixin; GLENN, Joseph
Patent: WO2012/68450 A1, 2012 ;
Location in patent: Page/Page column 201 ;
WO 2012/068450 A1
反应条件
potassium carbonate in acetone T=20 - 35°C; 18 h;
参考文献
AMGEN INC.
Patent: WO2008/130600 A2, 2008 ;
Location in patent: Page/Page column 53 ;
反应条件
1: in 2-butoxy-ethanol Heating; 2: With borane-THF
参考文献
ACS Medicinal Chemistry Letters, , vol. 2, # 12 p. 933 - 937
反应条件
1: sulfolane / 150 °C 2: borane-THF / tetrahydrofuran View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 20, # 9 p. 2845 - 2849
反应条件
1: With triethylamine; isobutyl chloroformate in tetrahydrofuran 0.5 h; Cooling with ice; 2: With sodium tetrahydroborate in tetrahydrofuran; water Cooling with ice;
参考文献
INCYTE CORPORATION; RODGERS, James D.; SHEPARD, Stacey; ZHU, Wenyu; SHAO, Lixin; GLENN, Joseph
Patent: WO2012/68450 A1, 2012 ;
Location in patent: Page/Page column 204-205 ;
WO 2012/068450 A1
参考文献
INCYTE CORPORATION; RODGERS, James D.; ARVANITIS, Argyrios G.
Patent: WO2013/26025 A1, 2013 ;
Location in patent: Page/Page column 138 ;
WO 2013/026025 A1
反应条件
1: With 2,4-dimethoxy-benzylamine
T=100°C;
2: With trifluoroacetic acid
0.5 h;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED; CHUAQUI, Claudio, Edmundo; HUANG, Shan; IOANNIDIS, Stephanos; SHI, Jie; SU, Mei; SU, Qibin
Patent: WO2010/38060 A1, 2010 ;
Location in patent: Page/Page column 77 ;
WO 2010/038060 A1
反应条件
in methanol
48 h; Heating / reflux;
参考文献
Blackaby, Wesley Peter; Castro Pineiro, Jose Luis; Lewis, Richard Thomas; Naylor, Elizabeth Mary; Street, Leslie Joseph
Patent: US2006/276655 A1, 2006 ;
Location in patent: Page/Page column 24 ;
US 20060276655 A1
反应条件
1: With triethylamine; isobutyl chloroformate in tetrahydrofuran
0.5 h; Cooling with ice;
2: With sodium tetrahydroborate in tetrahydrofuran; water
Cooling with ice;
参考文献
INCYTE CORPORATION; RODGERS, James D.; SHEPARD, Stacey; ZHU, Wenyu; SHAO, Lixin; GLENN, Joseph
Patent: WO2012/68450 A1, 2012 ;
Location in patent: Page/Page column 204-205 ;
WO 2012/068450 A1
