N-[(3R,6S)-6-(2,3-二氟苯基)六氢-2-氧代-1-(2,2,2-三氟乙基)-1H-氮杂卓-3-基]-4-(2,3-二氢-2-氧代-1H-咪唑并[4,5-b]吡啶-1-基)-1-哌啶甲酰胺合成路线 （共 5 条）
反应条件
1: (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one; chloroformic acid 4-nitrophenyl ester With triethylamine in tetrahydrofuran T=0°C; 0.5 h; 2: 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride With triethylamine in tetrahydrofuran; dichloromethane T=0 - 20°C; 48 h;
参考文献
WO2004/92166 A2, ;
Page 130 ;
WO 2004/092166 A2
反应条件
1: (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one; chloroformic acid 4-nitrophenyl ester With triethylamine in tetrahydrofuran T=0°C; 2: 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride With triethylamine in tetrahydrofuran; chloroform T=25°C;
参考文献
Burgey, Christopher S.; Paone, Daniel V.; Shaw, Anthony W.; Deng, James Z.; Nguyen, Diem N.; Potteiger, Craig M.; Graham, Samuel L.; Vacca, Joseph P.; Williams, Theresa M.
Organic Letters, 2008 , vol. 10, # 15 p. 3235 - 3238
反应条件
triethylamine in tetrahydrofuran; tert-butyl methyl ether T=20 - 60°C; 5 h; Product distribution / selectivity;
参考文献
Palucki, Michael; Davies, Ian; Steinbuebel, Dietrich; Rosen, Jonathan
Patent: US2009/124799 A1, 2009 ;
Location in patent: Page/Page column 2; 7-10 ;
US 20090124799 A1
反应条件
triethylamine in tetrahydrofuran T=60°C; Product distribution / selectivity;
参考文献
WO2007/120590 A2, ;
Page/Page column 18; 19; 22; 23-24 ;
WO 2007/120590 A2
反应条件
triethylamine in tetrahydrofuran T=20°C; 72 h;
参考文献
Journal of Medicinal Chemistry, , vol. 50, # 23 p. 5564 - 5567
