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    • 9. 发明授权
    • 1,4-Benzothiazines
    • 1,4-苯并噻嗪类
    • US4268301A
    • 1981-05-19
    • US28801
    • 1979-04-10
    • Tamon UematsuShunichi HashimotoHiromichi Oshio
    • Tamon UematsuShunichi HashimotoHiromichi Oshio
    • A01N37/24A01N39/04A01N43/84C07D279/16
    • A01N43/84A01N37/24A01N39/04C07D279/16
    • A process for producing novel 1,4-benzothiazine derivatives (I), ##STR1## (in which X is a halogen atom) and their derivatives, ##STR2## wherein R is a (C.sub.1 -C.sub.5) alkyl, (C.sub.3 -C.sub.6) cycloalkyl, phenyl, substituted phenyl, phenyl (C.sub.1 -C.sub.5) alkyl or phenoxy (C.sub.1 -C.sub.5) alkyl group, and herbicides containing these compounds as an active ingredient. Compound (I) is produced by the reaction between Compound (II) and phosphorus pentasulfide; Compound (II) is produced (1) by the reaction between an aminothiophenol (III), ##STR3## (in which X is a halogen atom), and a halogenated acetic acid, (2) by the ring closure of Compound (VI), (3) by the reduction and ring closure of Compound (VIII), and (4) by the hydrolysis and ring closure of Compound (X); Compound (VI) is produced by the reaction between Compound (III) and a halogenated acetyl halide; Compound (VIII) is produced by the oxidation of Compound (III) followed by reaction with a halogenated acetyl halide; and Compound (X) is produced by the reaction between Compound (III) and a halogenated acetic ester. Compounds (I), (II), (VI), (VIII) and (X) have a herbicidal activity.
    • (Ⅰ),(其中X是卤素原子)及其衍生物的新的1,4-苯并噻嗪衍生物(I)的制备方法,(VI) 其中R是(C 1 -C 5)烷基,(C 3 -C 6)环烷基,苯基,取代的苯基,苯基(C 1 -C 5)烷基或苯氧基(C 1 -C 5)烷基)的化合物,以及含有这些化合物的除草剂 作为活性成分。 化合物(I)通过化合物(II)和五硫化二磷之间的反应产生; 通过氨基苯硫酚(III),其中X是卤素原子,和卤代乙酸之间的反应产生(1)化合物(II),(2)通过化合物(VI)的闭环 ,(3)通过化合物(VIII)的还原和闭环,和(4)通过化合物(X)的水解和闭环; 化合物(VI)通过化合物(III)与卤化乙酰卤反应生成; 化合物(VIII)是通过化合物(III)的氧化反应生成的,然后与卤代乙酰卤反应; 化合物(X)通过化合物(III)与卤代乙酸酯的反应制备。 化合物(I),(II),(VI),(VIII)和(X)具有除草活性。