Methanesulfonyl chloride → HCID 57929943, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-(2,4-difluorophenyl)-5-(3-isopropyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-2-(piperidin-4-yl)thiazole (0.25 g, 0.57 mmol, Example #Q.1.1), TEA (0.32 mL, 2.3 mmol) and DCM (5 mL) was cooled to about 0-4° C. Methanesulfonyl chloride (0.044 mL, 0.57 mmol) was added. The reaction mixture was stirred at about 04° C. for about 1 h. The reaction was quenched with saturated aqueous Na2CO3 solution. The aqueous layer was extracted with DCM (200 mL). The organic layer was dried over Na2SO4, decanted, and concentrated. The crude product was purified by RP-HPLC (Table 1, Method e) to give the title compound (0.14 g, 48%): LC/MS (Table 1, Method a) Rt=2.49 min; MS m/z: 519.2 (M+H)+.

Provenance & Evidence