tert-Butanol → tert-butyl 2-(3-phenyl-1H-1,2,4-triazol-1-yl)ethylcarbamate

Participants

Reaction Conditions

Reaction Steps

A mixture of 3-(3-phenyl-1H-1,2,4-triazol-1-yl)propionoic acid (195 mg, 862 μmol), diphenyl phosphorazidate (242 μl, 1.12 mmol), triethylamine (240 μl, 1.72 mmol) in ter-butanol (33 mL) was heated at 50° C. for 5 h. Stirring was continued at 90° C. for another 12 h and all volatiles were removed in vacuo. The crude product was purified by preparative HPLC using an acetonitrile/water (containing 0.1% formic acid) gradient to afford the product as colorless oil (37 mg, 122 μmol, 14.1%). MS: M=289.1 (M+H)+

Provenance & Evidence