N-乙酰基-L-亮氨酰甘氨酰-N6-乙酰基-N-(4-甲基-2-氧代-2H-1-苯并吡喃-7-基)-L-赖氨酰胺合成路线 (共 5 条)
反应条件
N-ethyl-N,N-diisopropylamine in dichloromethane; acetonitrile
T=0 - 20°C; 1 h; Inert atmosphere;
参考文献
Madsen, Andreas S.; Olsen, Christian A.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5582 - 5590
反应条件
1: dichloromethane / 0.5 h / 20 °C
2: N-ethyl-N,N-diisopropylamine / dichloromethane; acetonitrile / 1 h / 0 - 20 °C / Inert atmosphere
View Scheme
参考文献
Madsen, Andreas S.; Olsen, Christian A.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5582 - 5590
反应条件
1.1: pyridine / tetrahydrofuran / 0.5 h / 0 °C
1.2: 2.67 h / 0 - 20 °C
2.1: piperidine / dichloromethane; acetonitrile / 24 h / 0 - 20 °C
3.1: benzotriazol-1-ol; diisopropyl-carbodiimide / dichloromethane / 0.17 h / Inert atmosphere
3.2: 1.17 h / 20 °C
4.1: dichloromethane / 0.5 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine / dichloromethane; acetonitrile / 1 h / 0 - 20 °C / Inert atmosphere
View Scheme
参考文献
Madsen, Andreas S.; Olsen, Christian A.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5582 - 5590
反应条件
1.1: benzotriazol-1-ol; diisopropyl-carbodiimide / dichloromethane / 0.17 h / 0 °C
1.2: 3.5 h
2.1: water; lithium hydroxide hydrate / tetrahydrofuran / 3 h / 20 °C
3.1: benzotriazol-1-ol; diisopropyl-carbodiimide / dichloromethane / 0.17 h / Inert atmosphere
3.2: 1.17 h / 20 °C
4.1: dichloromethane / 0.5 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine / dichloromethane; acetonitrile / 1 h / 0 - 20 °C / Inert atmosphere
View Scheme
参考文献
Madsen, Andreas S.; Olsen, Christian A.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5582 - 5590
反应条件
1.1: pyridine / tetrahydrofuran / 0.5 h / 0 °C
1.2: 2.67 h / 0 - 20 °C
2.1: piperidine / dichloromethane; acetonitrile / 24 h / 0 - 20 °C
3.1: benzotriazol-1-ol; diisopropyl-carbodiimide / dichloromethane / 0.17 h / Inert atmosphere
3.2: 1.17 h / 20 °C
4.1: dichloromethane / 0.5 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine / dichloromethane; acetonitrile / 1 h / 0 - 20 °C / Inert atmosphere
View Scheme
参考文献
Madsen, Andreas S.; Olsen, Christian A.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5582 - 5590