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    • 5. 发明授权
    • Process for preparing N-(3-amino-4-chlorophenyl) acylamides
    • 制备N-(3-氨基-4-氯苯基)酰胺的方法
    • US5663434A
    • 1997-09-02
    • US593726
    • 1996-01-29
    • Robert Joseph Maleski
    • Robert Joseph Maleski
    • C07C231/02C07C233/43C07C233/80C07C235/16C07C303/38C07C311/08C07C311/18C07C311/21C07C311/46
    • C07C231/02C07C303/38
    • The present invention provides a process for preparing N-(3-amino-4-chlorophenyl) acylamides of Formula I: ##STR1## comprising reacting, in a solvent comprising at least one polar solvent, in the presence of at least one acid acceptor, 1-chloro-2,4-diaminobenzene with at least one acyl chloride of formula I:Cl--X--Rwherein X is --CO-- or --SO.sub.2 --; R is selected from the group C.sub.1 -C.sub.25 alkyl; C.sub.1 -C.sub.25 alkyl substituted with one or more groups selected from C.sub.1 -C.sub.12 alkoxy, aryl, aryloxy and C.sub.5 -C.sub.7 cycloalkyl; aryl; C.sub.5 -C.sub.7 cycloalkyl. The present invention further comprises the step of purifying said N-(3-amino-4-chlorophenyl) acylamides by crystallizing from a non-polar solvent or conducting the reaction in a mixture of at least one polar and at least one non-polar solvent.
    • 本发明提供了制备式I的N-(3-氨基-4-氯苯基)酰胺的方法:包括在至少一种极性溶剂的溶剂中,在至少一种酸受体存在下, 具有式I的至少一种酰氯的1-氯-2,4-二氨基苯:其中X是-CO-或-SO 2 - ; R选自C 1 -C 25烷基; 被一个或多个选自C 1 -C 12烷氧基,芳基,芳氧基和C 5 -C 7环烷基的基团取代的C 1 -C 25烷基; 芳基; C5-C7环烷基。 本发明还包括通过从非极性溶剂中结晶或在至少一种极性和至少一种非极性溶剂的混合物中进行反应来纯化所述N-(3-氨基-4-氯苯基)酰胺的步骤 。