4-Methyl-5-((2R)-oxiran-2-yl)-2-benzofuran-1(3H)-one → 2-{4-[(2R)-2-Hydroxy-2-(4-methyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)ethyl]-2-oxopiperazin-1-yl}-7-methylquinoline-6-carbonitrile

Participants

Reaction Conditions

Reaction Steps

A mixture of 7-Methyl-2-(2-oxopiperazin-1-yl)quinoline-6-carbonitrile [I-3] (125 mg, 0.47 mmol) and 4-methyl-5-[(2R)-oxiran-2-yl]-2-benzofuran-1(3H)-one (134 mg, 0.70 mmol) in EtOH (1.5 mL) in a 5 mL microwave tube was heated to 140° C. for 20 minutes. LC showed formation of the desired product, which was purified by mass-directed reverse phase HPLC (AcCN-Water with 0.1% TFA). LC-MS (IE, m/z): 457 [M+1]+.

Provenance & Evidence