Methanesulfonyl chloride → Hydrochloric Acid

Participants

Reaction Steps

Compound 163 (32 mg, 0.056 mmol) was dissolved in 3 mL NMP. To it were added DIEA (60 μL, 0.34 mmol) and then methanesulfonyl chloride (13 μL, 0.17 mmol). The reaction was quenched in 20 m using TFA (0.1 mL). The mixture was directly subjected to reverse phase preparative HPLC to isolate (R)-5-(3-(4-methoxybenzamido)piperidin-1-yl)-3-(4-(1-(methylsulfonyl)piperidin-4-yl)phenylamino)pyrazine-2-carboxamide (173) as HCl salt. MS found for C30H37N7O5S as (M+H)+ 608.2, (M−H)− 606.3. UV: λ=304, 335, 372 nm.

Provenance & Evidence