2-硼酸基-5-[(4-甲基-1-哌嗪基)磺酰基]-1H-吲哚-1-羧酸叔丁酯合成路线 (共 6 条)
反应条件
1: 5-(4-methyl-piperazine-1-sulfonyl)-indole-1-carboxylic acid tert-butyl ester With tert.-butyl lithium
2: boric acid trimethyl ester in tetrahydrofuran
T=-78°C;
参考文献
Fraley, Mark E.; Arrington, Kenneth L.; Buser, Carolyn A.; Ciecko, Patrice A.; Coll, Kathleen E.; Fernandes, Christine; Hartman, George D.; Hoffman, William F.; Lynch, Joseph J.; McFall, Rosemary C.; Rickert, Keith; Singh, Romi; Smith, Sheri; Thomas, Kenneth A.; Wong, Bradley K.
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 351 - 355
反应条件
1.1: 100 percent / Et3N / CH2Cl2
2.1: 73 percent / ClSO3H; SOCl2
3.1: NaOH
4.1: 95 percent / MnO2 / CH2Cl2
5.1: 100 percent / DMAP
6.1: t-BuLi
6.2: 94 percent / tetrahydrofuran / -78 °C
View Scheme
参考文献
Fraley, Mark E.; Arrington, Kenneth L.; Buser, Carolyn A.; Ciecko, Patrice A.; Coll, Kathleen E.; Fernandes, Christine; Hartman, George D.; Hoffman, William F.; Lynch, Joseph J.; McFall, Rosemary C.; Rickert, Keith; Singh, Romi; Smith, Sheri; Thomas, Kenneth A.; Wong, Bradley K.
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 351 - 355
反应条件
1.1: 73 percent / ClSO3H; SOCl2
2.1: NaOH
3.1: 95 percent / MnO2 / CH2Cl2
4.1: 100 percent / DMAP
5.1: t-BuLi
5.2: 94 percent / tetrahydrofuran / -78 °C
View Scheme
参考文献
Fraley, Mark E.; Arrington, Kenneth L.; Buser, Carolyn A.; Ciecko, Patrice A.; Coll, Kathleen E.; Fernandes, Christine; Hartman, George D.; Hoffman, William F.; Lynch, Joseph J.; McFall, Rosemary C.; Rickert, Keith; Singh, Romi; Smith, Sheri; Thomas, Kenneth A.; Wong, Bradley K.
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 351 - 355
反应条件
1.1: NaOH
2.1: 95 percent / MnO2 / CH2Cl2
3.1: 100 percent / DMAP
4.1: t-BuLi
4.2: 94 percent / tetrahydrofuran / -78 °C
View Scheme
参考文献
Fraley, Mark E.; Arrington, Kenneth L.; Buser, Carolyn A.; Ciecko, Patrice A.; Coll, Kathleen E.; Fernandes, Christine; Hartman, George D.; Hoffman, William F.; Lynch, Joseph J.; McFall, Rosemary C.; Rickert, Keith; Singh, Romi; Smith, Sheri; Thomas, Kenneth A.; Wong, Bradley K.
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 351 - 355
反应条件
1.1: 95 percent / MnO2 / CH2Cl2
2.1: 100 percent / DMAP
3.1: t-BuLi
3.2: 94 percent / tetrahydrofuran / -78 °C
View Scheme
参考文献
Fraley, Mark E.; Arrington, Kenneth L.; Buser, Carolyn A.; Ciecko, Patrice A.; Coll, Kathleen E.; Fernandes, Christine; Hartman, George D.; Hoffman, William F.; Lynch, Joseph J.; McFall, Rosemary C.; Rickert, Keith; Singh, Romi; Smith, Sheri; Thomas, Kenneth A.; Wong, Bradley K.
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 351 - 355
反应条件
1.1: 100 percent / DMAP
2.1: t-BuLi
2.2: 94 percent / tetrahydrofuran / -78 °C
View Scheme
参考文献
Fraley, Mark E.; Arrington, Kenneth L.; Buser, Carolyn A.; Ciecko, Patrice A.; Coll, Kathleen E.; Fernandes, Christine; Hartman, George D.; Hoffman, William F.; Lynch, Joseph J.; McFall, Rosemary C.; Rickert, Keith; Singh, Romi; Smith, Sheri; Thomas, Kenneth A.; Wong, Bradley K.
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 351 - 355