Triethylamine → Voriconazole

Participants

Reaction Conditions

Reaction Steps

Voriconazole (1R)-(−)-10-camphorsulfonate from example 12 (11 g, 18.9 mmol, enantiomeric purity 100.0%) was suspended in deionised water (110 ml) and treated with triethylamine (2.90 ml, 20.8 mmol) at 45-55° C. for 3 hours. The suspension was cooled down to 20-25° C. and filtered. The cake was washed with deionised water (2×20 ml). The solid was dried under vacuum at 50-60° C. until constant weight (6.09 g, 92.13% yield).

Provenance & Evidence