3-氯-4-氨基三氟甲苯合成路线 （共 21 条）
反应条件
copper(I) oxide; hydrogenchloride; sodium nitrite 1.) from -5 deg C to 0 deg C, 10 min, 2.) H2O, from -5 deg C to RT, 60 min; Yield given. Multistep reaction;
参考文献
Tsuji; Nakamura; Konishi; Okumura; Matsuo
Chemical and Pharmaceutical Bulletin, 1992 , vol. 40, # 9 p. 2399 - 2409
反应条件
triethylamine in tetrahydrofuran
参考文献
Yang, Ling-Ling; Li, Guo-Bo; Ma, Shuang; Zou, Chan; Zhou, Shu; Sun, Qi-Zheng; Cheng, Chuan; Chen, Xin; Wang, Li-Jiao; Feng, Shan; Li, Lin-Li; Yang, Sheng-Yong
Journal of Medicinal Chemistry, 2013 , vol. 56, # 4 p. 1641 - 1655
反应条件
pyridine; hydrogen fluoride; sodium nitrite 1.) 0 deg C, 30 min; 2.) 130 deg C, 1 h; Yield given. Multistep reaction;
参考文献
Fukuhara, Tsuyoshi; Yoneda, Norihiko; Suzuki, Akira
Journal of Fluorine Chemistry, 1988 , vol. 38, p. 435 - 438
反应条件
1: With sulfuryl dichloride in 1-methyl-pyrrolidin-2-one; chlorobenzene T=55 - 60°C; 6 h; 2: With sodium hydroxide in 1-methyl-pyrrolidin-2-one; water; chlorobenzene Product distribution / selectivity;
参考文献
Gharda, Keki Hormusji
Patent: US2013/30190 A1, 2013 ;
Location in patent: Paragraph 0065 ;
反应条件
1: 92 percent / dimethylformamide / 10 h / 120 °C 2: 91 percent / SO2Cl2 / 2 h / 20 °C View Scheme
参考文献
Zhu, Lei; Zhang, Mingbao; Dai, Miao
Journal of Heterocyclic Chemistry, 2005 , vol. 42, # 4 p. 727 - 730
参考文献
Hatton; Leslie R.; Buntain; Ian G.; Hawkins; David W.; Parnell; Edgar W.; Pearson; Christopher J.; Roberts; David A.
Patent: US5232940 A1, 1993 ;
反应条件
1.1: sulfuryl dichloride; 1-methyl-pyrrolidin-2-one / 1-methyl-pyrrolidin-2-one; chlorobenzene / 8 h / 55 - 60 °C 2.1: nitrosyl-sulphuric acid; acetic acid / 30 - 55 °C 2.2: 0 - 15 °C 3.1: dichloromethane 4.1: boric acid; trichloroacetic acid; dihydrogen peroxide / chlorobenzene; water / 20 h / 15 - 20 °C View Scheme
参考文献
Gharda, Keki Hormusji
Patent: US2013/30190 A1, 2013 ;
反应条件
1.1: sulfuryl dichloride; 1-methyl-pyrrolidin-2-one / 1-methyl-pyrrolidin-2-one; chlorobenzene / 8 h / 55 - 60 °C 2.1: nitrosyl-sulphuric acid; acetic acid / 30 - 55 °C 2.2: 0 - 15 °C 3.1: dichloromethane View Scheme
反应条件
1.1: sulfuryl dichloride; 1-methyl-pyrrolidin-2-one / 1-methyl-pyrrolidin-2-one; chlorobenzene / 8 h / 55 - 60 °C 2.1: nitrosyl-sulphuric acid; acetic acid / 30 - 55 °C 2.2: 0 - 15 °C View Scheme
参考文献
Gharda, Keki Hormusji
Patent: US2013/30190 A1, 2013 ;
反应条件
in tetrahydrofuran
T=70°C; 23 h;
参考文献
CONVERGENCE PHARMACEUTICALS LIMITED; BESWICK, Paul John; GLEAVE, Robert James; HACHISU, Shuji; VILE, Sadie; BERTHELEME, Nicolas; WARD, Simon E
Patent: WO2012/4604 A1, 2012 ;
Location in patent: Page/Page column 40-41 ;
WO 2012/004604 A1
