反应详情

To 250 mg of toluene-4-sulfonic acid (S)-2-tert-butoxycarbonylamino-4-methyl-pentyl ester in 2.5 ml acetone and 0.5 ml water were added 112 mg of potassium carbonate, followed by the addition of 75 mg 4H-1,2,4-triazole-3-thiol. The reaction was heated in a microwave reactor for 5 min to 100° C. The pH was then adjusted to 7 by the addition of 2 M aqueous hydrochloric acid and the mixture was extracted with ethyl acetate twice. The combined organic phases were dried over sodium sulphate and concentrated in vacuo. 161 mg (80%) of [(S)-3-Methyl-1-(4H-[1,2,4]triazol-3-ylsulfanylmethyl)-butyl]-carbamic acid tert-butyl ester were obtained.

1. temperatureThe reaction was heated in a microwave reactor for 5 min to 100° C
2. extractionthe mixture was extracted with ethyl acetate twice
3. dry with materialThe combined organic phases were dried over sodium sulphate
4. concentrationconcentrated in vacuo