Oxalyl chloride → 4-(5-{6-[2-(Methoxymethyl)pyrrolidin-1-yl]-5-methylpyridin-3-yl}-1,2,4-oxadiazol-3-yl)benzenesulfonamide

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Reaction Steps

Oxalyl chloride (122 mL; 1.44 mmol), Intermediate 29 (120 mg; 0.48 mmol), 4-(aminosulfonyl)-N′-hydroxybenzenecarboximidamide, prepared as described in WO 2006/013104 A1 from 4-cyanobenzene-1-sulfonamide (ABCR; CD10716), (103 mg; 0.48 mmol, 1 eq.) and DIEA (248 mL; 1.44 mmol) were reacted according to the procedure described for Example 38. Purification by column chromatography (from cHex/EtOAc, 50/50 to EtOAc) followed by recrystallisation from DCM/n-pentane afforded the title compound as a yellow solid. LC/MS (Method A): 430.3 (M+H)+. HPLC (Method A) Rt 2.80 min (purity 93.1%).

Provenance & Evidence