N-((1R,3s,5S)-8-苄基-8-氮杂二环[3.2.1]辛烷-3-基)异丁酰胺合成路线 （共 14 条）
反应条件
1: exo-N-(8-benzyl-8-azabicyclo[3.2.1]oct-3-yl)-2-methylpropanamide With phosphorus pentachloride in dichloromethane T=0 - 20°C; 2 h; 2: acetic acid hydrazide in dichloromethane; pentan-1-ol T=10 - 20°C; 3: With acetic acid in dichloromethane; ethyl acetate T=80°C; 1 h;
参考文献
Auspex Pharmaceuticals, Inc.
Patent: US2008/146605 A1, 2008 ;
Location in patent: Page/Page column 41 ;
反应条件
1: exo-N-(8-benzyl-8-azabicyclo[3.2.1]oct-3-yl)-2-methylpropanamide With phosphorus pentachloride in dichloromethane T=-5 - 20°C; 4 h; Inert atmosphere; 2: oxalic acid monohydrazide in 1,1-dimethylpropan-1-ol; acetonitrile T=10 - 20°C; 15.5 h; Inert atmosphere; 3: With oxalic acid monohydrazide in 1,1-dimethylpropan-1-ol; acetonitrile T=80°C; 2 h; Inert atmosphere;
参考文献
Haycock-Lewandowski, Sarah J.; Wilder, Alexander; Ahman, Jens
Organic Process Research and Development, 2008 , vol. 12, # 6 p. 1094 - 1103
反应条件
1: PCl5 / CH2Cl2 / 0 °C 2: CH2Cl2; 2-methyl-butan-2-ol 3: p-TsOH / toluene / Heating View Scheme
参考文献
Asano, Shigehiro; Gavrilyuk, Julia; Burton, Dennis R.; Barbas, Carlos F.
ACS Medicinal Chemistry Letters, 2014 , vol. 5, # 2 p. 133 - 137
反应条件
1: phosphorus pentachloride / dichloromethane / 2 h / 0 - 20 °C / |Inert atmosphere
2: dichloromethane; 1,1-dimethylpropan-1-ol / 0 - 20 °C / |Inert atmosphere
3: acetic acid / ethyl acetate / 0.5 h / 80 °C / |Inert atmosphere
4: palladium 10 on activated carbon; hydrogen / methanol / 20 °C / 2585.81 Torr / |Inert atmosphere
View Scheme
参考文献
Asano, Shigehiro; Gavrilyuk, Julia; Burton, Dennis R.; Barbas, Carlos F.
ACS Medicinal Chemistry Letters, 2014 , vol. 5, # 2 p. 133 - 137
