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Amine to Amide



Example 1

To a mixture of the acid (0.3 g, 0.85 mmol) and BOP (442 mg, 1 mmol) in DMF at 0 C was added TEA (0.3 mL 2.14 mmol). The resulting mixture was stirred for 5 min, after which time the amine (110 mg, 1 mmol) in DMF was added dropwise and the reaction was stirred at RT for 5 h. The mixture was diluted with H2O and stirred overnight. The resulting solids were filtered and purified by chromatography (3% MeOH/CHCl3) to provide the product. [70 mg]

[Patent Reference: WO2010038081, page 133, (33.8 MB)]