Triphenylphosphine → HCID 178520986, compound

Participants

Reaction Steps

To a mixture of 200 mg (0.75 mmol) of cis-(4-cyclobutyl-piperazin-1-yl)-(4-hydroxy-cyclohexyl)-methanone, 133 mg (0.83 mmol) of 4-(1,2,4-triazole-1-yl)phenol, 241 mg (0.92 mmol) of triphenylphosphine in 1.5 ml of THF, a mixture of 212 mg (0.92 mmol) of di-tert-butyl azodicarboxylate in 1.5 ml of THF was added dropwise at 0° C., and stirred for 72 h at room temperature. After evaporation, the residue was purified by column chromatography on silica gel elating with CH2Cl2 and methanol=from 99:1 to 9:1. After that, the residue was purified by column chromatography on NH2-coating silica gel eluting % with CH2Cl2 and ethyl acetate=from 100:0 to 99:2. The combined product fractions were evaporated to dryness to yield 35 mg (11%) of the title compound. MS (m/e): 410.3 (MH+).

Provenance & Evidence