Methanesulfonic Acid → HCID 86594556, compound

Participants

Reaction Steps

To a room temperature solution of N1-(cyanomethyl)-N2-[3-(4-[4-(tert-butoxycarbonyl)piperazin-1-yl]phenyl)isoxazol-4-yl]leucinamide (15.5 mg, 0.031 mmol) in THF (2 mL) was added 8 equivalents of methanesulfonic acid (10% solution in dichloromethane) over 28 h. The reaction mixture was quenched with aqueous NaHCO3 solution and extracted with dichloromethane (3×). The organic phase was filtered through cotton and evaporated. Purification by flash chromatography (2% to 15% methanol/dichloromethane+0.5% ammonium hydroxide) gave 3.8 mg of N1-(cyanomethyl)-N2-[3-(4-piperazin-1-ylphenyl)isoxazol-4-yl]leucinamide. MS (+ESI): 397.4 [M+1]+.

Provenance & Evidence