Oxalic Acid → HCID 71522658, compound

Participants

Reaction Steps

At 0° C., 1-[2-(2-{(methoxymethyl)[(trimethylsilyl)methyl]amino}ethyl)phenyl]piperidin-2-one a5-2 (696 mg, 2 mmol, 2 eq) is slowly added to 2-ethenyl-4-methyl-1,3-thiazole a5-3 (125 mg, 1 mmol, 1 eq) diluted in dichloromethane/TFA (90 μl/10 μl). The mixture is stirred at room temperature overnight. Solvent is removed under reduced pressure and the residue is purified by basic reverse phase chromatography on silicagel (gradient: acetonitrile/H2O/NH4OH from 30/70/0.1 to 60/40/0.1 in 10 minutes). The product is dissolved in a minimum of acetone and oxalic acid (1 eq) is added to form the salt that is filtered, washed with diethyl ether and dried under vacuum to afford 215 mg of 1-(2-{2-[3-(4-methyl-1,3-thiazol-2-yl)pyrrolidin-1-yl]ethyl}phenyl)piperidin-2-one oxalate 87.

Provenance & Evidence