| 摘要 |
PURPOSE:To suppress the formation of a dimer and simply obtain an isothiazolecarboxamide derivative useful as an agrochemical, etc., in high yield by reacting a halogenoisothiazole which is a starting raw material with CO and amines using a specific catalyst. CONSTITUTION:This method for producing the objective compound expressed by formula II (R<1> and R<2> each is H, an alkyl, etc.; R<3> and R<4> each is H, an alkenyl, etc.) is to react an isothiazole derivative expressed by formula I (X is Br or I) with carbon monoxide and amines expressed by the formula R<3>R<4>NH in the presence of a palladium compound [preferably palladium(II) chloride, etc.] and a phosphine compound (e.g. tributylphosphine) as catalysts and a base (e.g. Na0H). Specifically, when, e.g. 5-iodo-3-methylisothiazole is used as the compound expressed by formula I nd n-octylamine is used as the compound expressed by formula I methylisothiazole-5-carboxamide is obtained. Furthermore, the phosphine compound is preferably used in an amount of 10-50 equiv. based on 1 equiv. palladium compound. |
