反应条件
1: N-methylmorpholine, isobutyl chloroformate / 1.) DMF, 20 min, 2.) DMF, RT, 18 h
2: H2 / 5percent Pd/C / methanol / 18 h / 1292.9 Torr
3: 2.) N-methylmorpholine / 1.) methanol, reflux, 1 h, 2.) methanol, 2 h
4: 94.8 percent / 1N HCl, trifluoroacetic acid / 55 °C
5: sodium dithionite / dimethylformamide; H2O / 0.5 h
6: 0.1N NaOH / 1.5 h
7: Me2SO / dimethylformamide / 47 h
8: 0.1N NaOH / acetonitrile
View Scheme
参考文献
Nair; Bridges; Henkel; Kisliuk; Gaumont; Sirotnak
Journal of Medicinal Chemistry, 1981 , vol. 24, # 9 p. 1068 - 1073