4-(4-乙基哌嗪-1-甲基)-3-三氟甲基苯胺合成路线 （共 6 条）
反应条件
palladium on activated charcoal; hydrogen in methanol
T=20°C; 12 h;
参考文献
HANMI PHARM CO., LTD.; BAE, In Hwan; SON, Jung Beom; HAN, Sang Mi; KWAK, Eun Joo; KIM, Ho Seok; SONG, Ji Young; BYUN, Eun Young; JUN, Seung Ah; AHN, Young Gil; SUH, Kwee Hyun
Patent: WO2013/100632 A1, 2013 ;
Location in patent: Page/Page column 37 ;
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
反应条件
1: 4-amino-2-trifluoromethylbenzaldehyde With hydrogenchloride in water; ethyl acetate; toluene
T=20 - 25°C; 0.0833333 h; Large scale;
2: N-ethyl-piperazine With pyridinium p-toluenesulfonate in ethyl acetate
T=76 - 78°C; Large scale;
3: With sodium tris(acetoxy)borohydride in ethyl acetate
Large scale;
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
反应条件
1: N-ethyl-N,N-diisopropylamine / dichloromethane / 3 h / 20 °C
2: palladium on activated charcoal; hydrogen / methanol / 12 h / 20 °C
View Scheme
参考文献
HANMI PHARM CO., LTD.; BAE, In Hwan; SON, Jung Beom; HAN, Sang Mi; KWAK, Eun Joo; KIM, Ho Seok; SONG, Ji Young; BYUN, Eun Young; JUN, Seung Ah; AHN, Young Gil; SUH, Kwee Hyun
Patent: WO2013/100632 A1, 2013 ;
反应条件
1: N-bromosuccinmide; 2,2'-azo-bisisobutyronitrile / 1,2-dichloro-ethane / 12 h / 80 °C
2: N-ethyl-N,N-diisopropylamine / dichloromethane / 3 h / 20 °C
3: palladium on activated charcoal; hydrogen / methanol / 12 h / 20 °C
View Scheme
参考文献
HANMI PHARM CO., LTD.; BAE, In Hwan; SON, Jung Beom; HAN, Sang Mi; KWAK, Eun Joo; KIM, Ho Seok; SONG, Ji Young; BYUN, Eun Young; JUN, Seung Ah; AHN, Young Gil; SUH, Kwee Hyun
Patent: WO2013/100632 A1, 2013 ;
反应条件
1.1: diisobutylaluminium hydride / tetrahydrofuran; toluene / 0.08 h / |Inert atmosphere; |Large scale
2.1: hydrogenchloride / toluene; ethyl acetate; water / 0.08 h / 20 - 25 °C / |Large scale
2.2: 76 - 78 °C / |Large scale
2.3: |Large scale
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
