2-氯-5-氨基三氟甲苯合成路线 （共 49 条）
反应条件
1: 91 percent
2: 97 percent / HCl (6N) / acetone / Heating
View Scheme
参考文献
Link; Stohler
European Journal of Medicinal Chemistry, 1984 , vol. 19, # 3 p. 261 - 265
反应条件
N-iodo-succinimide in tetrahydrofuran; methanol
参考文献
Lanter, James C.; Fiordeliso, James J.; Allan, George F.; Musto, Amy; Hahn, Do Won; Sui, Zhihua
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 21 p. 5646 - 5649
反应条件
1: NIS; p-TsOH / methanol; tetrahydrofuran
2: pyridine / Heating
3: aq. NaOH / methanol
View Scheme
参考文献
Lanter, James C.; Fiordeliso, James J.; Allan, George F.; Musto, Amy; Hahn, Do Won; Sui, Zhihua
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 21 p. 5646 - 5649
参考文献
Le Baut; Sparfel; Clairc; et al.
European Journal of Medicinal Chemistry, 1983 , vol. 18, # 5 p. 441 - 445
反应条件
zinc oxide
T=70°C; 10 h;
参考文献
Ahn, Hyemi; Lee, Jun A.; Kim, Hwan; Oh, Chang-Hyun; Lee, So Ha; Sim, Taebo; Hah, Jung-Mi; Kim, Dong Jin; Yoo, Kyung Ho
Bulletin of the Korean Chemical Society, 2011 , vol. 32, # 4 p. 1209 - 1214
反应条件
pyridine; phosphorus trichoride in toluene
12 h; Inert atmosphereReflux;
参考文献
Kang, Sunghyun; Min, Hye-Jin; Kang, Min-Seo; Jung, Myung-Geun; Kim, Semi
Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1748 - 1751
反应条件
hydrogenchloride; sodium acetate; sodium nitrite
1.) water; 2.) ethanol-water, 0 deg C, 3 h, overnight; Multistep reaction;
参考文献
Cocco; Maccioni; Plumitallo
Farmaco, Edizione Scientifica, 1985 , vol. 40, # 4 p. 272 - 284
反应条件
1: 4-methyl-morpholine / chloroform / 25 h / 5 - 65 °C / |Reflux
2: dichloromethane / 16 h / 20 °C
3: trifluoroacetic acid; triethylsilane / dichloromethane / 16 h / 50 °C
4: sulfuric acid / water / 3 h / |Reflux
View Scheme
参考文献
SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.; Feng, Weidong; Gao, Xiaoyong; Dai, Xiaojun
Patent: US2013/35492 A1, 2013 ;
反应条件
1.1: triethylamine / tetrahydrofuran / 4 h / 0 - 20 °C
2.1: n-butyllithium / tetrahydrofuran / 3 h / 0 °C
2.2: 3 h / 0 °C
3.1: 1-methyl-pyrrolidin-2-one / 36 h / 220 °C / Inert atmosphere
4.1: hydrogenchloride; ethanol / 12 h / 80 °C
View Scheme
参考文献
RADIUS HEALTH, INC.; MILLER, Chris, P.
Patent: WO2012/47617 A1, 2012 ;
WO 2012/047617 A1
