Tetrahydrofuran → HCID 58187754, compound

Participants

Reaction Steps

In a nitrogen atmosphere, intermediate 3 (100 mg, 0.264 mmol) was dissolved in acetonitrile (4 ml), and Mesyl-Cl (32 μl, 0.411 mmol) and DIPEA (78 μl, 0.447 mmol) were added. The mixture was stirred at RT for 30 minutes. Potassium fluoride (154 mg, 2.64 mmol) was added, and the mixture was stirred for 1 h at 60° C. TBAF 1M in THF (529 μl, 0.529 mmol) was added, and the mixture is stirred at 60° C. for 4 hours. The reaction mixture was partitioned between water and AcOEt, the organic layer was separated, dried over Na2SO4 and concentrated. The crude was purified by silica gel flash chromatography (eluent DCM/AcOEt=1:1) to yield intermediate 28 (62 mg, 61.7% yield).

Provenance & Evidence