Triethylamine → Voriconazole

Participants

Reaction Conditions

Reaction Steps

Voriconazole (1R)-(−)-10-camphorsulfonate (1 g, 1.72 mmol, enantiomeric purity 97.18%) was suspended in deionised water (10 ml) and treated with triethylamine (0.24 ml, 1.72 mmol) at 45-55° C. for 3 hours and 30 minutes. The suspension was cooled down to 20-25° C., stirred for 10 minutes and filtered. The cake was washed with deionised water (2×10 ml). The solid was dried under vacuum at 50-55° C. until constant weight (0.47 g, 78.26% yield).

Provenance & Evidence