反应详情

A solution of the methyl 3-[2-(1-tert-butoxycarbonyl-piperidin-4-yloxy)-4-(pyrrolidin-1-yl)benzoylamino]-thiophene-2-carboxylate (3.8 g, 7.2 mmol) and EtOH (100 mL) was treated with a solution of KOH (0.88 g) in water (80 mL). The reaction mixture was refluxed overnight, quenched with glacial acetic acid (1.5 mL) and concentrated under vacuum. The resulting aqueous mixture was extracted with EtOAc (2×100 mL). The combined extracts were dried over MgSO4 and concentrated to give 3.5 g (6.8 mmol, 94%) of the acid as a foam.

1. temperatureThe reaction mixture was refluxed overnight
2. customquenched with glacial acetic acid (1.5 mL)
3. concentrationconcentrated under vacuum
4. extractionThe resulting aqueous mixture was extracted with EtOAc (2×100 mL)
5. dry with materialThe combined extracts were dried over MgSO4
6. concentrationconcentrated