4-氰基-5-[(氰基乙酰基)氨基]-N,N-二乙基-3-甲基-2-噻吩甲酰胺合成路线 (共 6 条)
反应条件
10 Pd/C; hydrogen in methanol
T=20°C; P=22502.3 Torr;
参考文献
Lawrence, Harshani R.; Martin, Mathew P.; Luo, Yunting; Pireddu, Roberta; Yang, Hua; Gevariya, Harsukh; Ozcan, Sevil; Zhu, Jin-Yi; Kendig, Robert; Rodriguez, Mercedes; Elias, Roy; Cheng, Jin Q.; Sebti, Said M.; Schonbrunn, Ernst; Lawrence, Nicholas J.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7392 - 7416
反应条件
1: With benzotriazol-1-ol in dichloromethane; N,N-dimethyl-formamide
72 h;
2: in dichloromethane; N,N-dimethyl-formamide
72 h;
3: With trifluoroacetic acid
T=20°C; 168 h;
参考文献
7TM PHARMA A/S
Patent: WO2003/87044 A2, 2003 ;
Location in patent: Page/Page column 43 ;
WO 03/087044 A2
反应条件
1: triethylamine / dichloromethane / 48 h / 20 °C / |Inert atmosphere
2: hydrogen; 10 Pd/C / methanol / 20 °C / 22502.3 Torr
View Scheme
参考文献
Lawrence, Harshani R.; Martin, Mathew P.; Luo, Yunting; Pireddu, Roberta; Yang, Hua; Gevariya, Harsukh; Ozcan, Sevil; Zhu, Jin-Yi; Kendig, Robert; Rodriguez, Mercedes; Elias, Roy; Cheng, Jin Q.; Sebti, Said M.; Schonbrunn, Ernst; Lawrence, Nicholas J.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7392 - 7416
反应条件
1: triethylamine / dichloromethane / 48 h / 20 °C / |Inert atmosphere
2: hydrogen; 10 Pd/C / methanol / 20 °C / 22502.3 Torr
View Scheme
参考文献
Lawrence, Harshani R.; Martin, Mathew P.; Luo, Yunting; Pireddu, Roberta; Yang, Hua; Gevariya, Harsukh; Ozcan, Sevil; Zhu, Jin-Yi; Kendig, Robert; Rodriguez, Mercedes; Elias, Roy; Cheng, Jin Q.; Sebti, Said M.; Schonbrunn, Ernst; Lawrence, Nicholas J.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7392 - 7416
反应条件
1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; 1-hydroxy-7-aza-benzotriazole / dichloromethane / 20 °C / |Inert atmosphere
2: hydrogenchloride / ethyl acetate
View Scheme
参考文献
Castor, Katherine J.; Liu, Zhaomin; Fakhoury, Johans; Hancock, Mark A.; Mittermaier, Anthony; Moitessier, Nicolas; Sleiman, Hanadi F.
Chemistry - A European Journal, 2013 , vol. 19, # 52 p. 17836 - 17845
反应条件
1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; 1-hydroxy-7-aza-benzotriazole / dichloromethane / 20 °C / |Inert atmosphere
2: hydrogenchloride / ethyl acetate
View Scheme
参考文献
Castor, Katherine J.; Liu, Zhaomin; Fakhoury, Johans; Hancock, Mark A.; Mittermaier, Anthony; Moitessier, Nicolas; Sleiman, Hanadi F.
Chemistry - A European Journal, 2013 , vol. 19, # 52 p. 17836 - 17845