| 摘要 |
<p>PURPOSE:To provide a new (E)-2-aryl-3-fluoroacrylic acid useful as an intermedi ate compound for the synthesis of a fluoramine derivative having enzyme inhibiting action. CONSTITUTION:A compound of the formula I [Ar is (substituted) aromatic group], e.g. (E)-2-(4-methoxyphenyl)-3-fluoroacrylic acid. The compound can be produced by the hydrogenative decomposition of a 2-aryl-2- difluoromethylmalonic acid diester of the formula II (R is univalent organic group decomposable by hydrogenative decomposition) in a solvent in the presence of a catalyst preferably Raney-nickel, palladium-carbon, etc., in hydrogen atmosphere. A fluoramine derivative having enzyme inhibiting action can be synthesized by reducing the compound of the formula I or its ester and converting the hydroxyl group of the resultant alcohol to amino group.</p> |
