反应详情

This example illustrates the preparation of the compounds of formula I wherein X is --SOR1. In this example a mixture of 20 g. of 2-ethylthio-5-[2-(bicyclo[2.2.1]hept-7-yl)ethylaminocarbonyl]thiazole (0.064 mole); 40 ml. of 30% aqueous hydrogen peroxide and 200 ml. of acetic acid is stirred at a temperature of from 40° to 50° C for 4 hours. The mixture is concentrated by evaporation of a large portion of the acetic acid, under vacuum, at room temperature (about 20° C) and the resulting residue poured into 500 ml. of ethyl acetate and then washed with aqueous sodium bicarbonate solution until no acetic acid is present in the organic layer. The ethyl acetate layer is then separated, dried with anhydrous magnesium sulfate, filtered, and the resulting filtrate evaporated to dryness, under vacuum, affording 2-ethylsulfinyl-5-[2-(bicyclo[2.2.1]hept-7-yl)ethylaminocarbonyl]thiazole.

1. customthe preparation of the compounds of formula I wherein X
2. concentrationThe mixture is concentrated by evaporation of a large portion of the acetic acid, under vacuum, at room temperature (about 20° C)
3. additionthe resulting residue poured into 500 ml
4. washof ethyl acetate and then washed with aqueous sodium bicarbonate solution until no acetic acid
5. customThe ethyl acetate layer is then separated
6. dry with materialdried with anhydrous magnesium sulfate
7. filtrationfiltered
8. customthe resulting filtrate evaporated to dryness, under vacuum