Jm. Villalgordo et H. Heimgartner, A NOVEL SYNTHESIS OF 2,2-DISUBSTITUTED 3-AMINO-2H-AZIRINES BASED ON THE REACTION BETWEEN AMIDE ENOLATES AND DIPHENYL PHOSPHOROCHLORIDATE, Helvetica Chimica Acta, 76(8), 1993, pp. 2830-2837
A novel synthesis of 2,2-disubstituted 3-amino-2H-azirines based on th
e reaction between amide enolates and diphenyl phosphorochloridate (DP
PCl), followed by treatment with NaN3 is presented. The yields obtaine
d in general are excellent, and the method is suitable for laboratory-
scale preparations as well as for larger amounts.