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Amine to Amide



Example 1

To a solution of the amine (B) (33 mg, 0.070 mmol) and the acid (A) (35.9 mg, 0.280 mmol) in THF (3 mL) at 0 C was added DCC (57.8 mg, 0.280 mmol). The resulting mixture was stirred at RT for 2 days. The solvent was removed in vacuo and the crude material was taken up in EtOAc and washed with sat aq NaHCO3, 1N HCl, and brine. The org layer was dried (MgSO4) and concentrated. The residue was purified by Prep HPLC  to provide the product. [28 mg, 69%]

[Patent Reference: WO2015191681, page 77, (6.2 MB)]