5-氨基-2-甲基三氟甲苯合成路线 （共 7 条）
反应条件
potassium phosphate in 1-methyl-pyrrolidin-2-one T=90°C; 4 h;
参考文献
WO2007/104538 A1, ;
Page/Page column 64 ;
WO 2007/104538 A1
反应条件
tetrakis(triphenylphosphine) palladium(0); potassium carbonate in N,N-dimethyl-formamide T=115 - 120°C; Suzuki-Miyaura coupling; 17 h;
参考文献
Gray; Andrews; Hook; Kitteringham; Voyle
Tetrahedron Letters, 2000 , vol. 41, # 32 p. 6237 - 6240
反应条件
1: With hydrogen fluoride; SbF5 T=-20 - 0°C; 0.5 h; 2: With pyridine; hydrogen fluoride T=-78 - 0°C;
参考文献
Debarge, Sebastien; Violeau, Bruno; Bendaoud, Nohair; Jacquesy, Jean-Claude
Tetrahedron Letters, 2003 , vol. 44, # 9 p. 1747 - 1750
反应条件
1: 4-methyl-3-(trifluoromethyl)aniline With hydrogenchloride; sodium nitrite in acetic acid
T=-15 - -5°C; 0.166667 h;
2: sulfur dioxide With copper(l) chloride in acetic acid
0.666667 h;
3: in acetic acid
T=0°C; 0.75 h;
参考文献
AMGEN, INC.; ARRAY BIOPHARMA, INC.
Patent: WO2004/92164 A1, 2004 ;
Location in patent: Page 123 ;
WO 2004/092164 A1
反应条件
iodine cloride; sodium hydrogencarbonate in methanol; dichloromethane
T=20°C; 3 h;
参考文献
ELI LILLY AND COMPANY
Patent: WO2006/2342 A1, 2006 ;
Location in patent: Page/Page column 66 ;
反应条件
1: sodium carbonate / water; 1,4-dioxane / 20 °C
2: N-bromosuccinmide; 2,2'-azo-bisisobutyronitrile / tetrachloromethane / |Reflux
3: triethylamine / tetrahydrofuran / 50 °C
4: trifluoroacetic acid / dichloromethane / 1 h / 20 °C
View Scheme
参考文献
Li, Yupeng; Shen, Mengjie; Zhang, Zhang; Luo, Jinfeng; Pan, Xiaofen; Lu, Xiaoyun; Long, Huoyou; Wen, Donghai; Zhang, Fengxiang; Leng, Fang; Li, Yingjun; Tu, Zhengchao; Ren, Xiaomei; Ding, Ke
Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 10033 - 10046
反应条件
1: pyridine / dichloromethane
2: 2,2'-azo-bisisobutyronitrile; N-bromosuccinmide / tetrachloromethane / |Irradiation
View Scheme
参考文献
Shieh, Wen-Chung; Mckenna, Joe; Sclafani, Joseph A.; Xue, Song; Girgis, Michael; Vivelo, James; Radetich, Branko; Prasad, Kapa
Organic Process Research and Development, 2008 , vol. 12, # 6 p. 1146 - 1155
