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    • 3. 发明授权
    • Process for producing halogenated heteroaryl compounds
    • 卤化杂芳基化合物的制备方法
    • US6114524A
    • 2000-09-05
    • US319642
    • 1999-06-08
    • Shigemitsu OkadaRyosuke UshijimaKiyofumi Ishikawa
    • Shigemitsu OkadaRyosuke UshijimaKiyofumi Ishikawa
    • C07D213/61C07D213/79C07D213/85C07D215/48C07D241/44C07D213/02C07D215/18C07D215/20C07D237/12C07D237/14
    • C07D213/79C07D213/61C07D213/85C07D215/48C07D241/44
    • The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group. The compound is prepared by reacting a compound represented by the formula (I): ##STR2## with a quaternary ammonium halide in the presence of phosphorus pentoxide.
    • PCT No.PCT / JP97 / 04508 Sec。 371 1999年6月8日第 102(e)日期1999年6月8日PCT 1997年12月9日PCT公布。 第WO98 / 25906号公报 日期:1998年6月18日本发明涉及式(II)表示的化合物的制造方法:其中,X为卤素原子,A1,A2和A3各自相同或不同,选自碳原子数 或氮原子,条件是至少A1,A2或A3为氮原子。 R 1,R 2,R 3和R 4各自相同或不同,选自氢原子,低级烷基,氰基,羧基,低级烷氧基羰基,卤素原子和硝基。 还提供其中R 1和R 2彼此相邻,R 1和R 2可以彼此组合以形成5-或6-元环,其可以在其环上带有一个选自以下的取代基: 低级烷基,腈基,羧基,低级烷氧基羰基,氨基甲酰基,卤素原子,硝基和氨基 - (低级烷基)基。 该化合物通过在五氧化二磷存在下使式(I)表示的化合物与季铵卤化物反应来制备。