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5-[3-(morpholin-4-yl)prop-1-yn-1-yl]thiophene-2-sulfonamide[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
60%
With bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide; triethylamine; In ethyl acetate; at 50℃; for 1h;Inert atmosphere;
General procedure: Pd(PPh3)2Cl2 (26.2 mg, 0.1 mmol) and CuI (9.5 mg,0.05 mmol) were added to triethylamine (1 ml) under argonatmosphere and stirred for 5 min. Then a solution of5-bromo-2-thiophene sulfonamide (1) (242 mg, 1 mmol) inEtOAc (5 ml) and the appropriate tertiary propargylamine(2 mmol) were added. The reaction mixture was stirred for1 h at 50 under inert atmosphere. The reaction mixturewas then cooled, diluted with EtOAc, and treated with a fewdrops of aqueous ammonia, stirred for 5-10 min and filteredthrough a thin layer of silica gel. The solution was evaporatedto dryness and the product was isolated by silica gel columnchromatography (eluent CH2Cl2-EtOAc-MeOH). In order toobtain hydrochlorides, the isolated product was dissolvedin 1:1 EtOAc-Et2O mixture and treated with anhydrousethereal HCl solution to pH 1. The mixture was stirred untilthe reaction was complete (TLC control), evaporated todryness, and diluted with anhydrous ether. The precipitatewas collected by filtration and dried.
Chemistry
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