反应条件
1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine / dichloromethane / 20 °C
2: piperidine / N,N-dimethyl-formamide / 0.33 h / 20 °C
3: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; 1,2-dichloro-ethane / dichloromethane / 20 °C
4: trifluoroacetic acid; 2-[(2-Hydroxy-1,1-bis[hydroxymethyl]ethyl)amino]ethanesulfonic acid / dichloromethane / 2 h
5: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 48 h / 20 °C
View Scheme
参考文献
Wu, Li-Chuan; Wen, Zhe-Sheng; Qiu, Ya-Tao; Chen, Xiao-Qin; Chen, Hao-Bin; Wei, Ming-Ming; Liu, Zi; Jiang, Sheng; Zhou, Guang-Biao
ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 10 p. 921 - 926