Potassium Carbonate → tert-butyl 2-(4-(N-(2-morpholinoethyl)methylsulfonamido)-1,3-dioxoisoindolin-2-yl)acetate

Participants

Reaction Conditions

Reaction Steps

A mixture of tert-butyl 2-(4-(methylsulfonamido)-1,3-dioxoisoindolin-2-yl)acetate (196 mg, 0.553 mmol) (prepared with an analogous procedure to that described in, Example 29, Scheme 29, Steps 1, 2, 3, 4 for the preparation of Compound 160), 4-(2-chloroethyl)morpholine hydrochloride (108 mg, 0.581 mmol), and K2CO3 (168 mg, 1.217 mmol) in acetonitrile (10 ml) was stirred at 75° C. overnight. The solvent was removed under vacuum, and the residue was taken up in a EtOAc/DCM/Et2O mixture and filtered through Na2SO4 to remove the inorganic salts. After evaporation of the solvent, tert-butyl 2-(4-(N-(2-morpholinoethyl)methylsulfonamido)-1,3-dioxoisoindolin-2-yl)acetate was obtained (256 mg, 0.548 mmol, 99% yield, MS/ESI+ 467 [MH]+).

Provenance & Evidence