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    • 4. 发明授权
    • Method for substitution of an amino group of a primary amine by a
chlorine atom and a synthetic method by application thereof
    • 用氯原子取代伯胺氨基的方法及其应用的合成方法
    • US5811555A
    • 1998-09-22
    • US749775
    • 1996-11-20
    • Takashi WakasugiTadashi MiyakawaTakayuki Tanonaka
    • Takashi WakasugiTadashi MiyakawaTakayuki Tanonaka
    • C07D277/32
    • C07D277/32
    • This invention relates to methods for substitution of an amino group of a heterocyclic primary amine by a chlorine atom and synthesis of 2-chloro-5-methylthiazole and its derivatives by application thereof. Typically, a heterocyclic primary amine and sodium nitrite are caused to react in the presence of hydrochloric acid, followed by heating the formed diazonium base at 30.degree.-100.degree. C. in the presence of an equimolar or more of hydrochloric acid to substitute the amino group by the chlorine atom. Further, 2-amino-5-methylthiazole and sodium nitrite are caused to react in the presence of hydrochloric acid, followed by heating the formed diazonium base at 30.degree.-100.degree. C. in the presence of an equimolar or over of hydrochloric acid to give 2-chloro-5-methylthiazole. Then, the resultant 2-chloro-5-methylthiazole is caused to react with a chlorinating agent to give 2-chloro-5-chloro-methylthiazole.
    • 本发明涉及用氯原子取代杂环伯胺的氨基和通过其应用合成2-氯-5-甲基噻唑及其衍生物的方法。 通常,使杂环伯胺和亚硝酸钠在盐酸存在下反应,然后在等摩尔或更多的盐酸存在下,在30-100℃下加热形成的重氮基,以取代氨基 由氯原子组成。 此外,使2-氨基-5-甲基噻唑和亚硝酸钠在盐酸存在下反应,然后在等摩尔或过量盐酸存在下,在30-100℃下加热形成的重氮基, 得到2-氯-5-甲基噻唑。 然后,使得到的2-氯-5-甲基噻唑与氯化剂反应,得到2-氯-5-氯 - 甲基噻唑。