Methanesulfonamide → tert-Butyl-4-((4-chlorophenethyl)(4-((methylsulfonyl)carbamoyl)benzyl)amino)-piperidine-1-carboxylate

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

4-(((1-(tert-Butoxycarbonyl)piperidin-4-yl)(4-chlorophenethyl)amino)methyl)benzoic acid synthesized in Step 2 was dissolved in DCM (5 mL/mmol) and DIPEA (3 equiv) and methanesulfonamide (2 eqs) were added. The reaction mixture was cooled to 0° C. and TFFH (1.2 eq) was added in one portion. The reaction mixture was stirred at 0° C. for 6 hours and then for 15 hours at room temperature. Ethyl acetate (15 mL/mmol) was added and the solution was washed sequentially with 5% citric acid (2×), 5% NaHCO3 (2×) and brine (2×) and was dried over MgSO4. The drying agent was filtered off and the solvents were evaporated in vacuo. The crude product was purified by silica gel chromatography.

Herkunft & Nachweise