Réaction #67281

ord-17a5df4cda5c49fea3146204156f6994

Conditions de réaction

Conditions détaillées
See reaction.notes.procedure_details.

Traitement

  1. 1
    Lavagethe resulting mixture was washed with HCl (1 N) and brine
  2. 2
    SéchageThe organic phase was dried (Na2SO4)
  3. 3
    Autreevaporated to dryness

Mode opératoire

A solution of [5-fluoro-7-(methylsulfonyl)-2,3-dihydro-1,4-benzodioxin-2-yl]methanol (0.4 g, 1.7 mmol), toluenesulfonyl chloride (0.5 g, 2.6 mmol), TEA (0.4 ml, 2.6 mmol) and 4-DMAP (0.2 g, 1.7 mmol) in DCM (10 ml) was stirred at rt for 1 h. DCM was added and the resulting mixture was washed with HCl (1 N) and brine. The organic phase was dried (Na2SO4) and evaporated to dryness to give the title compound (0.7 g). MS m/z (rel. intensity, 70 eV) 416 (M+, 31), 244 (bp), 243 (26), 231 (19), 91 (70).

Source

DOI: 10.6084/m9.figshare.5104873.v1Brevet: US08524766B2uspto-grants-2013_09