NEW SALICYLIC ACID DERIVATIVE AND SALICYLIC ACID-BASED COMPOUND AND ANTIFUNGAL AGENT

摘要

PURPOSE: To obtain a new compound exhibiting selectively excellent antifungal activity against fungi, hardly exhibiting toxicity to human and animals, scarcely having adverse effect, safe and useful as an antifungal agent applicable to a wide range of mycotic infections. ;CONSTITUTION: This compound is expressed by formula I (R¹ is H or an alkoxyalkyl; R² is a lower alkoxy, an amino, etc.; X is a halogen or a halogen- substituted phenyl; Y is a halogen or H), e.g. 3,3-dichloro-4-ethyl-1-(3- methoxymethoxy-4-methoxycarbonylphenyl)-2-pyrrolidinone. The compound is preferably obtained by reductively subjecting a salicylic acid-based compound of formula II (Z is Cl or Br) to cyclization reaction with a cyclization agent such as tributyltinhydride, Furthermore, the compound of formula II is preferably obtained by reacting, e.g. an alkyl 4-amino-2-alkoxyalkoxybenzoate with an alkyl 1-halogenated-2-butene to afford a new compound of formula III and reacting the compound with trichloroacetyl chloride, etc.;COPYRIGHT: (C)1996,JPO