反应详情

tert-butyl 5-chloro-4-[(2-cyclopentyl-6-methyl-5-oxo-2,6,9,11-tetrazabicyclo[5.4.0]undeca-7,9,11-trien-10-yl)amino]-2-fluoro-benzoate (Intermediate 220; 220 mg, 0.45 mmol) was dissolved in DCM (7.5 mL) and trifluoroacetic acid (2.5 mL) added. The mixture was stirred at room temperature for 2 hours. The refraction mixture was evaporated, the residue dissolved in methanol/DCM and absorbed on to an SCX column, which was subsequently washed with methanol and eluted with ammonia in methanol. Product containing fractions were combined and evaporated to yield the title compound as a white solid (195 mg, 100%).

1. customThe refraction mixture was evaporated
2. dissolutionthe residue dissolved in methanol/DCM
3. customabsorbed on to an SCX column, which
4. washwas subsequently washed with methanol
5. washeluted with ammonia in methanol
6. additionProduct containing fractions
7. customevaporated