Vinyl Acetate → (1R)-1-[5-(3-chlorophenyl)isoxazol-3-yl]ethyl acetate

Participants

Reaction Steps

The title compound of Example 7.1 (106.5 g, 476 mmol) and Novozyme 435® (13 g) are taken up under Ar in dry toluene (1.5 L). After addition of vinyl acetate (66 mL, 716 mmol) the reaction was run at RT over night, followed by filtration over diatomaceous earth and washing with DCM. The solvent was evaporated in vacuo and the crude product was subjected to column chromatography on silica using dichloromethane/methanol (20:1) to give the title compound (50 g, 47%).

Provenance & Evidence