PRODUCTION OF SULFONE DERIVATIVE

PURPOSE:To safely, inexpensively and simply obtain a sulfone derivative useful as an antifungal agent without employing a heavy metal catalyst by reacting a sulfide or sulfoxide compound with an oxidizing agent under an acidic condition. CONSTITUTION:A compound of formula I [R1, R2 are H, alkyl, cyc...

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Hauptverfasser: SHIMAKO KOZO, OHASHI NAOHITO, FUJIMOTO KOJI
Format: Patent
Sprache:eng
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Zusammenfassung:PURPOSE:To safely, inexpensively and simply obtain a sulfone derivative useful as an antifungal agent without employing a heavy metal catalyst by reacting a sulfide or sulfoxide compound with an oxidizing agent under an acidic condition. CONSTITUTION:A compound of formula I [R1, R2 are H, alkyl, cycloalkyl, cycloalkylmethyl, alkenyl, heterocyclic group, aryl or aralkyl which may be substituted with a substituent (halogen, NO2, alkyl, alkoxy, phenyl, phenoxy, benzyl, benzyloxy, etc.); R4-R7 are H, alkyl, alkenyl, aryl which may be substituted with the same substituent as the above substituent; Az is 1,2,4- triazol-1-(or 4)-yl, imidazolyl; n is 0, 1] is reacted with an oxidizing agent such as hydrogen peroxide or hypochlorous acid under an acidic condition using hydrochloric acid, methanesulfonic acid, p-toluenesulfonic acid, etc., to produce a sulfone derivative of formula II.