4-Toluenesulfonyl chloride → Acetic acid (S)-2-tert-butoxycarbonylamino-1-[5-(4-trifluoromethoxy-phenyl)-1,3,4-oxadiazol-2-yl]-butyl ester

Participants

Reaction Conditions

Reaction Steps

acetic acid (S)-2-tert-butoxycarbonylamino-1-[N′-(4-trifluoromethoxy-benzoyl)-hydrazinocarbonyl]-butyl ester (0.21 mmol, 0.1 g) is dissolved in THF (5 mL) and the solution filled into a Smith Microwave synthesizer reaction vessel. 2-tert-Butylimino-2-diethylamino-1,3-dimethylperhydro-1,2,3-diazaphosphorine on polystyrene (1.05 mmol, 0.456 g, 2.3 mmol/g loading) and the p-Toluenesulfonic chloride (0.25 mmol, 0.048 g) are added and the reaction mixture heated at 150° C. for 10 min (fixed hold time) in the microwave synthesizer.

Provenance & Evidence