4,4-二氟-N-((1S)-3-羟基-1-苯基丙基)环己烷甲酰胺合成路线 (共 3 条)
反应条件
N-ethyl-N,N-diisopropylamine; HATU in N,N-dimethyl-formamide
T=18 - 25°C; 144 h;
参考文献
ASTRAZENECA AB
Patent: WO2006/1752 A1, 2006 ;
Location in patent: Page/Page column 70 ;
WO 2006/001752 A1
反应条件
sodium tetrahydroborate in methanol
T=0°C; 0.166667 h;
参考文献
Zhao, Gui-Ling; Lin, Shuangzheng; Korotvicka, Ales; Deiana, Luca; Kullberg, Martin; Cordova, Armando
Advanced Synthesis and Catalysis, 2010 , vol. 352, # 13 p. 2291 - 2298
反应条件
1: sodium carbonate / water; dichloromethane; toluene / 1 h / 20 - 35 °C / |Inert atmosphere; |Large scale
2: sodium tetrahydroborate / methanol; tetrahydrofuran / 2.5 h / 50 °C / |Inert atmosphere; |Reflux; |Large scale
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参考文献
Ahman, Jens; Birch, Melissa; Haycock-Lewandowski, Sarah J.; Long, James; Wilder, Alexander
Organic Process Research and Development, 2008 , vol. 12, # 6 p. 1104 - 1113