(S)-1-(5-氟嘧啶-2-基)乙胺盐酸盐合成路线 （共 4 条）
反应条件
hydrogenchloride in 1,4-dioxane; dichloromethane
T=20°C; 3 h;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2008/129255 A1, 2008 ;
Location in patent: Page/Page column 72 ;
WO 2008/129255 A1
反应条件
hydrogenchloride in 1,4-dioxane
T=20°C; 3 h; Product distribution / selectivity;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2007/49041 A1, 2007 ;
Location in patent: Page/Page column 73 ;
WO 2007/049041 A1
反应条件
1: (S)-1-phenyl-ethylamine; potassium dihydrogenphosphate; pyridoxal 5'-phosphate; potassium carbonate; acetic acid; ω-transaminase / water; toluene / 18 h / 29 °C / pH 7.5 / |Enzymatic reaction
2: potassium carbonate / 2-methyl tetrahydrofuran; water / 18 h / 40 °C
3: hydrogenchloride / isopropyl alcohol / 24 h / 40 °C
View Scheme
参考文献
Frodsham, Lianne; Golden, Michael; Hard, Susan; Kenworthy, Martin N.; Klauber, David J.; Leslie, Kevin; Macleod, Claire; Meadows, Rebecca E.; Mulholland, Keith R.; Reilly, Julie; Squire, Christopher; Tomasi, Simone; Watt, Denise; Wells, Andrew S.
Organic Process Research and Development, 2013 , vol. 17, # 9 p. 1123 - 1130
反应条件
1.1: tetrahydrofuran; 2-methyl tetrahydrofuran / -40 °C
1.2: -25 °C
2.1: (S)-1-phenyl-ethylamine; potassium dihydrogenphosphate; pyridoxal 5'-phosphate; potassium carbonate; acetic acid; ω-transaminase / water; toluene / 18 h / 29 °C / pH 7.5 / |Enzymatic reaction
3.1: potassium carbonate / 2-methyl tetrahydrofuran; water / 18 h / 40 °C
4.1: hydrogenchloride / isopropyl alcohol / 24 h / 40 °C
View Scheme
参考文献
Frodsham, Lianne; Golden, Michael; Hard, Susan; Kenworthy, Martin N.; Klauber, David J.; Leslie, Kevin; Macleod, Claire; Meadows, Rebecca E.; Mulholland, Keith R.; Reilly, Julie; Squire, Christopher; Tomasi, Simone; Watt, Denise; Wells, Andrew S.
Organic Process Research and Development, 2013 , vol. 17, # 9 p. 1123 - 1130
