1H-吡咯并[3,2-b]吡啶-2-羧酰胺合成路线 （共 11 条）
反应条件
ammonia in water
T=20°C; Product distribution / selectivity;
参考文献
Aventis Pharmaceuticals Inc.
Patent: US2005/131012 A1, 2005 ;
Location in patent: Page/Page column 15 ;
US 20050131012 A1
反应条件
ammonia; water
T=60°C; P=1034.32 Torr; 5 h;
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
反应条件
1.1: sodium ethanolate / tetrahydrofuran / 10 - 20 °C / Large scale reaction
1.2: 2 h / 20 °C
2.1: palladium 10 on activated carbon; ammonium formate; acetic acid / ethanol; water / 3.25 h / 35 °C / Large scale reaction
3.1: ammonia / ethylene glycol / 6.92 h / 25 - 65 °C
View Scheme
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
反应条件
1.1: pivalic acid sodium salt / 1-methyl-pyrrolidin-2-one / 2.75 h / 20 - 50 °C / Large scale reaction
2.1: sulfuric acid; water / 50 - 100 °C / Large scale reaction
3.1: sodium ethanolate / tetrahydrofuran / 10 - 20 °C / Large scale reaction
3.2: 2 h / 20 °C
4.1: palladium 10 on activated carbon; ammonium formate; acetic acid / ethanol; water / 3.25 h / 35 °C / Large scale reaction
5.1: ammonia / ethylene glycol / 6.92 h / 25 - 65 °C
View Scheme
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
反应条件
1: palladium 10 on activated carbon; ammonium formate; acetic acid / ethanol; water / 3.25 h / 35 °C / Large scale reaction
2: ammonia / ethylene glycol / 6.92 h / 25 - 65 °C
View Scheme
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
反应条件
1.1: sulfuric acid; water / 50 - 100 °C / Large scale reaction
2.1: sodium ethanolate / tetrahydrofuran / 10 - 20 °C / Large scale reaction
2.2: 2 h / 20 °C
3.1: palladium 10 on activated carbon; ammonium formate; acetic acid / ethanol; water / 3.25 h / 35 °C / Large scale reaction
4.1: ammonia / ethylene glycol / 6.92 h / 25 - 65 °C
View Scheme
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
反应条件
1.1: sodium ethanolate / tetrahydrofuran / 10 - 20 °C / Large scale reaction
1.2: 2 h / 20 °C
2.1: palladium 10 on activated carbon; ammonium formate; acetic acid / ethanol; water / 3.25 h / 35 °C / Large scale reaction
3.1: ammonia; water / 5 h / 60 °C / 1034.32 Torr
View Scheme
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
反应条件
1.1: pivalic acid sodium salt / 1-methyl-pyrrolidin-2-one / 2.75 h / 20 - 50 °C / Large scale reaction
2.1: sulfuric acid; water / 50 - 100 °C / Large scale reaction
3.1: sodium ethanolate / tetrahydrofuran / 10 - 20 °C / Large scale reaction
3.2: 2 h / 20 °C
4.1: palladium 10 on activated carbon; ammonium formate; acetic acid / ethanol; water / 3.25 h / 35 °C / Large scale reaction
5.1: ammonia; water / 5 h / 60 °C / 1034.32 Torr
View Scheme
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
反应条件
1: palladium 10 on activated carbon; ammonium formate; acetic acid / ethanol; water / 3.25 h / 35 °C / Large scale reaction
2: ammonia; water / 5 h / 60 °C / 1034.32 Torr
View Scheme
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
反应条件
1.1: sulfuric acid; water / 50 - 100 °C / Large scale reaction
2.1: sodium ethanolate / tetrahydrofuran / 10 - 20 °C / Large scale reaction
2.2: 2 h / 20 °C
3.1: palladium 10 on activated carbon; ammonium formate; acetic acid / ethanol; water / 3.25 h / 35 °C / Large scale reaction
4.1: ammonia; water / 5 h / 60 °C / 1034.32 Torr
View Scheme
参考文献
Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045
