反应详情

(RS)-[1-Amino-1-[4-({2-methoxy-2-[l -(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yl]-acetylamino }-methyl)-phenyl]-meth-(E)-ylidene]-carbamic acid benzyl ester (0.5 g) was heated in 5 N HCl (20 ml) to 50° C. and stirring at that temperature was continued for 4 h. After cooling to r.t., the mixture was washed with EtOAc and cooled to 0° C. The pH was brought to ˜12 by the dropwise addition of 4 N NaOH. The mixture was then extracted with EtOAc. The combined organics were washed with brine, dried (MgSO4), filtered and concentrated to give (RS)-[1-amino-1-(4-{[2-(1H-benzoimidazol-2-yl)-2-methoxy-acetylamino]-methyl}-phenyl)-meth-(E)-ylidene]-carbamic acid benzyl ester (0.258 g) as light yellow solid. MS472.3 ([M+H]+)

1. washthe mixture was washed with EtOAc
2. temperaturecooled to 0° C
3. additionThe pH was brought to ˜12 by the dropwise addition of 4 N NaOH
4. extractionThe mixture was then extracted with EtOAc
5. washThe combined organics were washed with brine
6. dry with materialdried (MgSO4)
7. filtrationfiltered
8. concentrationconcentrated