申请人:Kureha Chemical Industry Co., Ltd.
公开号:US05811555A1
公开(公告)日:1998-09-22
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.
本发明涉及一种通过将杂环初级胺的氨基替换为氯原子并应用其合成2-氯-5-甲基噻唑及其衍生物的方法。通常,在盐酸存在下使杂环初级胺和亚硝酸钠反应,然后在等摩尔或更多的盐酸存在下将形成的重氮基在30℃-100℃加热,以替换氨基为氯原子。进一步,在盐酸存在下使2-氨基-5-甲基噻唑和亚硝酸钠反应,然后在等摩尔或超过等摩尔的盐酸存在下将形成的重氮基在30℃-100℃加热,得到2-氯-5-甲基噻唑。然后,将得到的2-氯-5-甲基噻唑与氯化剂反应,得到2-氯-5-氯甲基噻唑。