6,11-二氢-N-[3-(4-吗啉)丙基]-5-氧代-5H-茚并[1,2-c]异喹啉-9-磺酰胺合成路线 （共 5 条）
反应条件
triethylamine in dichloromethane
T=20°C; 24 h;
参考文献
Inotek Pharmaceutical, Corp.
Patent: US2006/19980 A1, 2006 ;
Location in patent: Page/Page column 31-33; 54 ;
反应条件
1: 4-(3-aminopropyl)-morpholine With sodium hydrogencarbonate in water; ethyl acetate
0.25 h;
2: 9-chlorosulfonyl-5,6-dihydro-5-oxo-indeno[1,2-c]isoquinoline in water; ethyl acetate
T=20°C; 24 h; Product distribution / selectivity;
参考文献
INOTEK PHARMACEUTICALS CORPORATION
Patent: WO2005/82368 A1, 2005 ;
Location in patent: Page/Page column 60; 86-87 ;
反应条件
1: 88 percent / triethylsilane; trifluoroacetic acid / 96 h / 20 °C
2: 92 percent / chlorosulfonyl chloride / 2 h / 20 °C
3: 56 percent / Et3N / CH2Cl2 / 24 h / 20 °C
View Scheme
参考文献
Jagtap, Prakash G.; Baloglu, Erkan; Southan, Garry J.; Mabley, Jon G.; Li, Hongshan; Zhou, Jing; Van Duzer, John; Salzman, Andrew L.; Szabo, Csaba
Journal of Medicinal Chemistry, 2005 , vol. 48, # 16 p. 5100 - 5103
反应条件
1: 92 percent / chlorosulfonyl chloride / 2 h / 20 °C
2: 56 percent / Et3N / CH2Cl2 / 24 h / 20 °C
View Scheme
参考文献
Jagtap, Prakash G.; Baloglu, Erkan; Southan, Garry J.; Mabley, Jon G.; Li, Hongshan; Zhou, Jing; Van Duzer, John; Salzman, Andrew L.; Szabo, Csaba
Journal of Medicinal Chemistry, 2005 , vol. 48, # 16 p. 5100 - 5103
反应条件
1: 87 percent / triethylsilane; trifluoroacetic acid / 24 h / 20 °C
2: 92 percent / chlorosulfonyl chloride / 2 h / 20 °C
3: 56 percent / Et3N / CH2Cl2 / 24 h / 20 °C
View Scheme
参考文献
Jagtap, Prakash G.; Baloglu, Erkan; Southan, Garry J.; Mabley, Jon G.; Li, Hongshan; Zhou, Jing; Van Duzer, John; Salzman, Andrew L.; Szabo, Csaba
Journal of Medicinal Chemistry, 2005 , vol. 48, # 16 p. 5100 - 5103
