N-t-Boc-4,4-二氟-L-脯氨酰胺合成路线 （共 4 条）
反应条件
1: With pivaloyl chloride; triethylamine in dichloromethane
T=-15°C; 1 h;
2: With ammonia in dichloromethane; water
T=-15°C; 1 h;
参考文献
SANOFI-SYNTHELABO
Patent: WO2003/74500 A2, 2003 ;
Location in patent: Page/Page column 15-16 ;
反应条件
1.1: diethylamino-sulfur trifluoride; ethanol / dichloromethane / 18 h / 20 °C / |Inert atmosphere
2.1: potassium hydroxide
3.1: dicyclohexyl-carbodiimide; 1-hydroxy-pyrrolidine-2,5-dione / dichloromethane / 15 - 20 °C
3.2: 0.33 h / 20 °C
View Scheme
参考文献
UNIVERSITEIT ANTWERPEN; FOX CHASE CANCER CENTER; JANSEN, Koen; DE MEESTER, Ingrid; HEIRBAUT, Leen; CHENG, Jonathan D; JOOSSENS, Jurgen; AUGUSTYNS, Koen; VAN DER VEKEN, Pieter
Patent: WO2013/107820 A1, 2013 ;
反应条件
1.1: potassium hydroxide
2.1: dicyclohexyl-carbodiimide; 1-hydroxy-pyrrolidine-2,5-dione / dichloromethane / 15 - 20 °C
2.2: 0.33 h / 20 °C
View Scheme
参考文献
UNIVERSITEIT ANTWERPEN; FOX CHASE CANCER CENTER; JANSEN, Koen; DE MEESTER, Ingrid; HEIRBAUT, Leen; CHENG, Jonathan D; JOOSSENS, Jurgen; AUGUSTYNS, Koen; VAN DER VEKEN, Pieter
Patent: WO2013/107820 A1, 2013 ;
反应条件
1.1: 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical; trichloroisocyanuric acid / dichloromethane / 0 - 20 °C
2.1: diethylamino-sulfur trifluoride; ethanol / dichloromethane / 18 h / 20 °C / |Inert atmosphere
3.1: potassium hydroxide
4.1: dicyclohexyl-carbodiimide; 1-hydroxy-pyrrolidine-2,5-dione / dichloromethane / 15 - 20 °C
4.2: 0.33 h / 20 °C
View Scheme
参考文献
UNIVERSITEIT ANTWERPEN; FOX CHASE CANCER CENTER; JANSEN, Koen; DE MEESTER, Ingrid; HEIRBAUT, Leen; CHENG, Jonathan D; JOOSSENS, Jurgen; AUGUSTYNS, Koen; VAN DER VEKEN, Pieter
Patent: WO2013/107820 A1, 2013 ;
