Abstract:
PURPOSE: A process of preparing 2-phenyliminothiazoline derivatives and salts thereof by reacting isothiocyanate derivatives and phenylamine in an inactive organic solvent and then reacting the obtained phenylthiourea derivatives with gamma-halo-beta-ketoanilide derivatives in the presence of an inactive organic solvent is provided. Whereby, the compounds are useful as an agricultural germicide. CONSTITUTION: 2-phenyliminothiazoline derivatives of formula(I-a) show a fungicidal activity, in particular against rice blast disease. In formula, R1 and R2 are each alkyl expressed by H, methyl, ethyl, propyl, butyl, pentyl or hexyl, halo expressed by fluoro, chloro or bromo, alkoxy expressed by methoxy, ethoxy, propoxy, isopropoxy, butyl, isobutoxy or sec-butoxy, alkoxycarbonyl expressed by cyano, nitro, trifluoromethyl, trifluoromethoxy, methylthio, phenyl, phenoxy, methoxycarbonyl, ethoxycaronyl, propoxycarbonyl or isopropoxycarbonyl; R3 is alkyl expressed by H, methyl, ethyl, propyl, isopropyl, cyclopropyl, butyl, pentyl, cyclopentyl, hexyl, cyclohexyl or aryl, or cycloalkyl; and X is Cl or Br.
Abstract:
2-phenyliminothiazolines of the following formula I, their salts, their preparation method and their use for treating rice blast. The phenyliminothiazolines and their salts of the present invention have low toxicity to environment or living organisms, and exert high activity at low concentration for treating rice blast through a new control mechanism, that is by inhibiting pentaketide synthesis and cyclization of the melanin sythesis process in formula I