(S)-2-环己基-2-(吡嗪-2-羧酰胺)乙酸合成路线 （共 6 条）
反应条件
1.1: 1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / N,N-dimethyl-formamide / 72 h 2.1: sodium hydroxide / tetrahydrofuran; methanol / 0 - 20 °C 2.2: pH 3.5 View Scheme
参考文献
VERENIGING VOOR CHRISTELIJK HOGER ONDERWIJS, WETENSCHAPPELIJK ONDERZOEK EN PATIENTENZORG; RUIJTER, Eelco; ORRU, Romano; ZNABET, Anass; POLAK, Marloes; TURNER, Nicholas
Patent: WO2011/103932 A1, 2011 ;
反应条件
1.1: 1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / N,N-dimethyl-formamide / 72 h 2.1: sodium hydroxide / tetrahydrofuran; methanol / 0 - 20 °C 2.2: pH 3.5 3.1: dichloromethane / 72 h / 20 °C 4.1: potassium carbonate; methanol / 0.5 h / 20 °C 4.2: 20 °C View Scheme
反应条件
water; sodium hydroxide in tetrahydrofuran; methanol
T=20°C;
参考文献
VERENIGING VOOR CHRISTELIJK HOGER ONDERWIJS, WETENSCHAPPELIJK ONDERZOEK EN PATIENTENZORG; RUIJTER, Eelco; ORRU, Romano; ZNABET, Anass; POLAK, Marloes; TURNER, Nicholas
Patent: WO2011/103932 A1, 2011 ;
Location in patent: Page/Page column 43 ;
反应条件
1: 2-carboxypyrazine With 1,1'-carbonyldiimidazole in tetrahydrofuran
T=55 - 60°C; Inert atmosphere;
2: L-α-cyclohexylglycine potassium salt in tetrahydrofuran; tert-butyl alcohol
T=20°C; Inert atmosphere;
参考文献
DIPHARMA FRANCIS S.R.L.; MANTEGAZZA, Simone; ATTOLINO, Emanuele; ALLEGRINI, Pietro
Patent: WO2013/131978 A1, 2013 ;
Location in patent: Page/Page column 14 ;
反应条件
1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0 - 20 °C / Inert atmosphere
2: lithium hydroxide hydrate / tetrahydrofuran; water / 3 h / 0 °C
View Scheme
参考文献
Milo, Lawrence J.; Lai, Jack H.; Wu, Wengen; Liu, Yuxin; Maw, Hlaing; Li, Youhua; Jin, Zhiping; Shu, Ying; Poplawski, Sarah E.; Wu, Yong; Sanford, David G.; Sudmeier, James L.; Bachovchin, William W.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4365 - 4377
反应条件
1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0 - 20 °C / Inert atmosphere
2: lithium hydroxide hydrate / tetrahydrofuran; water / 3 h / 0 °C
View Scheme
参考文献
Milo, Lawrence J.; Lai, Jack H.; Wu, Wengen; Liu, Yuxin; Maw, Hlaing; Li, Youhua; Jin, Zhiping; Shu, Ying; Poplawski, Sarah E.; Wu, Yong; Sanford, David G.; Sudmeier, James L.; Bachovchin, William W.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4365 - 4377
