Ethyl propiolate → ethyl 1-{2-ethoxy-4-[(ethylamino)carbonyl]phenyl}-1H-1,2,3-triazole-4-carboxylate

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Reaction Steps

To a solution of 4-azido-3-ethoxy-N-ethylbenzamide (0.70 g) obtained in Example 131d) in toluene (30 ml) was added ethyl propiolate (0.61 ml), and the mixture was heated under reflux overnight under a nitrogen atmosphere. The reaction mixture was allowed to cool to room temperature, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column (ethyl acetate/hexane=1/1 to ethyl acetate) to give the title compound as a white powder (0.59 g, 60%).

Provenance & Evidence