(8S,9R)-5-氟-8-(4-氟苯基)-2,7,8,9-四氢-9-(1-甲基-1H-1,2,4-三唑-5-基)-3H-吡啶并[4,3,2-de]酞嗪-3-酮合成路线 （共 21 条）
反应条件
in acetone Product distribution / selectivity;
参考文献
WO2012/54698 A1, ;
Page/Page column 44-45; 54 ;
反应条件
1.1: 2-methyl tetrahydrofuran; triethylamine / dichloromethane / 0.17 h / |Large scale 1.2: 20 - 95 °C / |Large scale 2.1: hydrazine hydrate / tetrahydrofuran / 20 °C / |Inert atmosphere 2.2: 18 h / 60 °C 3.1: acetonitrile / 48 h / |Reflux; |Inert atmosphere 4.1: caesium carbonate / tetrahydrofuran / 4 h / 55 °C 5.1: CHIRALPAK IA / diethylamine; methanol / |Resolution of racemate View Scheme
反应条件
1.1: hydrazine hydrate / tetrahydrofuran / 20 °C / |Inert atmosphere 1.2: 18 h / 60 °C 2.1: acetonitrile / 48 h / |Reflux; |Inert atmosphere 3.1: caesium carbonate / tetrahydrofuran / 4 h / 55 °C 4.1: CHIRALPAK IA / diethylamine; methanol / |Resolution of racemate View Scheme
反应条件
1: acetonitrile / 48 h / |Reflux; |Inert atmosphere 2: caesium carbonate / tetrahydrofuran / 4 h / 55 °C 3: CHIRALPAK IA / diethylamine; methanol / |Resolution of racemate View Scheme
反应条件
1: caesium carbonate / tetrahydrofuran / 4 h / 55 °C 2: CHIRALPAK IA / diethylamine; methanol / |Resolution of racemate View Scheme
反应条件
1: hydrazine hydrate / methanol / 10 h / 25 °C 2: CHIRALPAK IA / diethylamine; methanol / |Resolution of racemate View Scheme
反应条件
1: 6 h / 40 °C 2: hydrazine hydrate / methanol / 10 h / 25 °C 3: CHIRALPAK IA / diethylamine; methanol / |Resolution of racemate View Scheme
反应条件
1: hydrazine hydrate / methanol / 20 °C 2: CHIRALPAK IA column / diethylamine; carbon dioxide; methanol / Resolution of racemate View Scheme
反应条件
1: acetonitrile / 48 h / Reflux; Inert atmosphere 2: caesium carbonate / tetrahydrofuran / 4 h / 55 °C 3: CHIRALPAK IA column / diethylamine; carbon dioxide; methanol / Resolution of racemate View Scheme
反应条件
1: caesium carbonate / tetrahydrofuran / 4 h / 55 °C 2: CHIRALPAK IA column / diethylamine; carbon dioxide; methanol / Resolution of racemate View Scheme
