4-Methyl-5-((2R)-oxiran-2-yl)-2-benzofuran-1(3H)-one → 6-Fluoro-3-({4-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)ethyl]-2-oxopiperazin-1-yl}acetyl)-2-methylbenzonitrile

Participants

Reaction Conditions

Reaction Steps

A mixture of 6-Fluoro-2-methyl-3-[(2-oxopiperazin-1-yl)acetyl]benzonitrile (40 mg, 0.14 mmol) and 4-methyl-5-[(2R)-oxiran-2-yl]-2-benzofuran-1(3H)-one (42 mg, 0.22 mmol) in EtOH (2 mL) was heated to 140° C. for 1 hour. The reaction mixture was concentrated to dryness, and dissolved in MeOH, filtered and shot into Mass-directed HPLC for separation to give the title product. LC-MS (IE, m/z): 466 [M+1]+.

Provenance & Evidence