反应条件
1: 82 percent / N,N-diisopropylethylamine DIEA, HOBt / dimethylformamide / 0 - 20 °C
2: H2 / 5percent Pd/C / acetic acid; propan-2-ol / 760 Torr / Ambient temperature
3: 75 percent / N-methylmorpholine hydrochloride / dimethylformamide / 4 h / -10 - 0 °C / '
4: H2 / 5percent Pd/C / acetic acid; propan-2-ol / 760 Torr / Ambient temperature
5: N-methylmorpholine NMM, N,N'-dicyclohexylcarbodiimide DCC, HOBt / dimethylformamide / 1.) 0 deg C, 2 h, 2.) RT, 24 h
6: trifluoroacetic acid TFA / CH2Cl2 / 1 h / 0 °C
View Scheme
参考文献
Lazarus, LH; Salvadori, S; Grieco, P; Wilson, WE; Tomatis, R
European Journal of Medicinal Chemistry, 1992 , vol. 27, # 8 p. 791 - 797