反应详情

A mixture of Intermediate 10 (80 mg, 0.210 mmol), 4-cyclopropyl-benzoyl chloride (J. Med. Chem., 52(14), 4329-4337; 2009) (76 mg, 0.421 mmol), and DMAP (2.6 mg, 0.021 mmol) in pyridine (2 ml) was stirred at r.t. overnight. The mixture was evaporated to dryness, then sat. aqueous NaHCO3 was added, and the mixture was extracted with DCM. The organic layer was dried, filtered, and evaporated to dryness. The residue was purified by flash chromatography (silica gel, EtOAc/MeOH/NH3 gradient) to obtain Example 20.

1. customThe mixture was evaporated to dryness
2. additionsat. aqueous NaHCO3 was added
3. extractionthe mixture was extracted with DCM
4. customThe organic layer was dried
5. filtrationfiltered
6. customevaporated to dryness
7. customThe residue was purified by flash chromatography (silica gel, EtOAc/MeOH/NH3 gradient)
8. customto obtain Example 20