Propargyl bromide → HCID 86662771, compound

Participants

Reaction Steps

150 mg (0.3 mmol) of 1-(2,2-difluoroethyl)-3-(2-iodophenyl)-1H-[1,3]thiazolo[4,5-c][1,2]thiazin-4-ol 2,2-dioxide (compound I-a-14) were dissolved in 3 ml of DMF, and 85 mg of potassium carbonate were added at RT. The reaction mixture was stirred at RT for 5 min, and then 0.035 ml (0.46 mmol) of propargyl bromide was added dropwise. The reaction mixture was stirred at 90° C. for 4 h, then poured onto water and extracted repeatedly with ethyl acetate. The combined organic phases were dried (sodium sulfate) and concentrated to dryness. The residue was purified by means of preparative HPLC(C18—SiO2, gradient acetonitrile/water 20:80 to 100:0). This gave 51 mg of compound I-h-3.

Provenance & Evidence