反应详情

温度

90 °C

A mixture of 4-(5-iodobenzoxazol-2-yl)piperazine-1-carboxylic acid benzyl ester, prepared in Example 2 (1.48 mmol theory), 1-napthalenethiol (0.237 g, 1.48 mmol), CuI (0.042 g, 0.22 mmol), and K2CO3 (0.409 g, 2.96 mmol) in isopropanol was heated at 90° C. overnight, diluted with 20% MeOH in CH2Cl2, and filtered through a pad of silica gel. The filtrate was concentrated to dryness. The resultant residue was purified by chromatography with 5% MeOH in CH2Cl2 to provide the title compound (230 mg, 31% overall yield from 4-benzoxazol-2-yl-piperazine-1-carboxylic acid benzyl ester), characterized by NMR and mass spectral analyses.

1. filtrationfiltered through a pad of silica gel
2. concentrationThe filtrate was concentrated to dryness
3. customThe resultant residue was purified by chromatography with 5% MeOH in CH2Cl2