tert-Butyl (3R)-3-(hydroxymethyl)piperazine-1-carboxylate → tert-butyl (3R)-4-[2-(3-cyano-4-fluoro-2-methylphenyl)-2-hydroxyethyl]-3-(hydroxymethyl)piperazine-1-carboxylate

関与物質

反応条件

反応手順

6-Fluoro-2-methyl-3-(2-oxiranyl)benzonitrile (prepared as described above, 4.80 g, 27.1 mmol) and (R)-4-N—BOC-2-hydroxymethyl-piperazine (8.79 g. 40.6 mmol) were suspended in EtOH (30 mL) and heated in a microwave apparatus at 150° C. for 1 h. The reaction mixture was cooled and evaporated to dryness. The residue was purified by chromatography through a 330 g ISCO Redi-sep column eluting with ethyl acetate to 5% MeOH/ethyl acetate to yield the title compound. LC-MS: M+1=394;

情報源と証拠