(S)-4-苄基-3-(氟甲基)吗啉合成路线 (共 4 条)
反应条件
1: With borane-THF in tetrahydrofuran T=0 - 20°C; 15 h; Inert atmosphere; 2: With water; sodium hydroxide in methanol 3 h; Reflux;
参考文献
MITSUBISHI TANABE PHARMA CORPORATION; SANOFI-AVENTIS; SAKAI, Daiki; NAKAYAMA, Kazuki; WATANABE, Kazutoshi
Patent: WO2011/19089 A1, 2011 ;
Location in patent: Page/Page column 20-21 ;
WO 2011/019089 A1
反应条件
1: With hexafluoropropene diethylamine in dichloromethane T=-30 - 20°C; 2 h; Inert atmosphere; 2: With sodium methylate in methanol 0.5 h;
参考文献
MEDIVIR AB; AYESA, Susana; BELDA, Oscar; BJÖRKLUND, Catarina; NILSSON, Magnus; RUSSO, Francesco; SAHLBERG, Christer; WIKTELIUS, Daniel
Patent: WO2013/95275 A1, 2013 ;
Location in patent: Page/Page column 49 ;
反应条件
1.1: sodium hydride / N,N-dimethyl-formamide; mineral oil / 1 h / Cooling with ice; Inert atmosphere 1.2: 5 h / 20 °C 2.1: borane-THF / tetrahydrofuran / 15 h / 0 - 20 °C / Inert atmosphere 2.2: 3 h / Reflux 3.1: triethylamine / dichloromethane / 1 h / 0 °C 3.2: 15 h / 20 °C 4.1: hydrogen; acetic acid / palladium on carbon / 4 h / 40 °C 5.1: [bis(2-methoxyethyl)amino]-sulfur trifluoride / dichloromethane / 8 h / 20 °C / Reflux 6.1: borane-THF / tetrahydrofuran / 15 h / 0 - 20 °C / Inert atmosphere 6.2: 3 h / Reflux View Scheme
参考文献
MITSUBISHI TANABE PHARMA CORPORATION; SANOFI-AVENTIS; SAKAI, Daiki; NAKAYAMA, Kazuki; WATANABE, Kazutoshi
Patent: WO2011/19089 A1, 2011 ;
WO 2011/019089 A1
反应条件
1.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 2 h / 20 °C 2.1: hexafluoropropene diethylamine / dichloromethane / 2 h / -30 - 20 °C / |Inert atmosphere 2.2: 0.5 h View Scheme
参考文献
MEDIVIR AB; AYESA, Susana; BELDA, Oscar; BJÖRKLUND, Catarina; NILSSON, Magnus; RUSSO, Francesco; SAHLBERG, Christer; WIKTELIUS, Daniel
Patent: WO2013/95275 A1, 2013 ;