4-[4-(三氟甲氧基)苯氧基]哌啶合成路线 （共 10 条）
反应条件
hydrogenchloride in water
参考文献
G. D. Searle and Company
Patent: US6372758 B1, 2002 ;
US 6372758 B1
反应条件
hydrogenchloride in 1,4-dioxane T=20°C; 3 h;
参考文献
Wang, Tiancai; Xin, Ting; Fan, Houxing; Chen, Yilang
Patent: US2013/143864 A1, 2013 ;
Location in patent: Paragraph 0105; 0106 ;
反应条件
di-isopropyl azodicarboxylate; triphenylphosphine in tetrahydrofuran T=20°C; Cooling with ice;
参考文献
Wang, Tiancai; Xin, Ting; Fan, Houxing; Chen, Yilang
Patent: US2013/143864 A1, 2013 ;
Location in patent: Paragraph 0090; 0091; 0092 ;
反应条件
hydrogen; acetic acid; palladium 10 on activated carbon T=90°C; P=30003 Torr; AutoclaveInert atmosphere;
参考文献
SALTIGO GMBH
Patent: US2010/152454 A1, 2010 ;
Location in patent: Page/Page column 3-4 ;
反应条件
potassium hydroxide; 2-methyl-propan-1-ol T=100°C; 2 h; Product distribution / selectivity;
参考文献
OTSUKA PHARMACEUTICAL CO., LTD.
Patent: WO2008/140090 A1, 2008 ;
Location in patent: Page/Page column 32-33 ;
反应条件
1.1: sodium hydride / N,N-dimethyl-formamide; mineral oil / 0.5 h / |Cooling with ice 1.2: 15 h / 20 °C 2.1: hydrogenchloride / 1,4-dioxane / 3 h / 20 °C View Scheme
参考文献
Wang, Tiancai; Xin, Ting; Fan, Houxing; Chen, Yilang
Patent: US2013/143864 A1, 2013 ;
反应条件
1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran; water / 20 °C 2: trifluoroacetic acid; water / 3 h / 20 °C View Scheme
参考文献
Shanghai Sun-Sail Pharmaceutical Science and Technology Co., Ltd; WANG, Tiancai; XIN, Ting; FAN, Houxing; CHEN, Yilang
Patent: EP2573090 A1, 2013 ;
反应条件
1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran; water / 20 °C 2: trifluoroacetic acid; water / 3 h / 20 °C View Scheme
参考文献
Shanghai Sun-Sail Pharmaceutical Science and Technology Co., Ltd; WANG, Tiancai; XIN, Ting; FAN, Houxing; CHEN, Yilang
Patent: EP2573090 A1, 2013 ;
反应条件
palladium/active carbon in ethanol
T=70 - 80°C; 9 h;
参考文献
OTSUKA PHARMACEUTICAL CO., LTD.
Patent: WO2005/92832 A1, 2005 ;
Location in patent: Page/Page column 48-49 ;
反应条件
1: 64 percent / Cs2CO3 / Pd(OAc)2; rac-BINAP / toluene / 0.5 h / Heating
2: 94 percent / EtOH / pyridinium p-toluenesulfonate / 24 h / 70 °C
View Scheme
参考文献
Sasaki, Hirofumi; Haraguchi, Yoshikazu; Itotani, Motohiro; Kuroda, Hideaki; Hashizume, Hiroyuki; Tomishige, Tatsuo; Kawasaki, Masanori; Matsumoto, Makoto; Komatsu, Makoto; Tsubouchi, Hidetsugu
Journal of Medicinal Chemistry, 2006 , vol. 49, # 26 p. 7854 - 7860
