6-氨基-1H-吡咯并[2,3-B]吡啶-5-羧酸乙酯合成路线 (共 2 条)
反应条件
1: ethyl ethynyl ether With benzo[1,3,2]dioxaborole in tetrahydrofuran; hexane
T=20 - 70°C; 3 h;
2: 2,6-diamino-5-iodo-nicotinic acid ethyl ester With sodium hydroxide; tetrakis(triphenylphosphine) palladium(0) in tetrahydrofuran; hexane
7.5 h; Heating / reflux;
3: With hydrogenchloride; sodium hydroxide
more than 3 stages;
参考文献
Eisai RandD Management Co., Ltd.
Patent: EP1782811 A1, 2007 ;
Location in patent: Page/Page column 62 ;
反应条件
1: ethyl ethynyl ether With benzo[1,3,2]dioxaborole in tetrahydrofuran; hexane
T=0 - 70°C; 3 h;
2: 2,6-diamino-5-iodo-nicotinic acid ethyl ester With sodium hydroxide; tetrakis(triphenylphosphine) palladium(0) in tetrahydrofuran; hexane
T=20°C; 7.5 h; Heating / reflux;
3: With hydrogenchloride in tetrahydrofuran; hexane; water
T=20°C; 60 h;
参考文献
Eisai Co., Ltd.
Patent: EP1669348 A1, 2006 ;
Location in patent: Page/Page column 70 ;