Triethylamine → [1-(1-Pyrimidin-2-yl-cyclopropyl-carbamoyl)-3-1,2,3-triazol-2-yl-propyl]-carbamic acid tert-butyl ester

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Reaction Steps

To a solution of the 2-tert-butoxycarbonylamino-4-1,2,3-triazol-2-yl-butyric acid (0.1 g, 0.37 mmol) in DMF (2 mL) was added 1-pyrimidin-2-yl-cyclopropylamine dihydrochloride (50 mg, 0.24 mmol) followed by Et3N (0.1 ml, 0.74 mmol) and HATU (211 mg, 0.55 mmol). The mixture was stirred at room temperature for 1 h. The mixture was diluted with water and EtOAc. The layers were separated and the organic layer was washed with water (3×30 mL), brine (2×30 mL), dried over MgSO4, filtered, and concentrated in vacuo to yield crude [1-(1-pyrimidin-2-yl-cyclopropyl-carbamoyl)-3-1,2,3-triazol-2-yl-propyl]-carbamic acid tert-butyl ester. The product was not purified and was used in subsequent reactions.

Provenance & Evidence