Metal salt catalyzed process to oxazolines and subsequent formation of
chloroketones
    14.
    发明授权
    Metal salt catalyzed process to oxazolines and subsequent formation of chloroketones 有权
    金属盐催化方法进行恶唑啉,随后形成氯代酮

    公开(公告)号:US6057477A

    公开(公告)日:2000-05-02

    申请号:US293119

    申请日:1999-04-16

    摘要: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichlorolsocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid to produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure. Additionally, when R is a hydrogen atom, a dichloroketone can be conveniently formed through adjustment of reaction conditions.

    摘要翻译: 本发明涉及一种制备α-氯代酮化合物的方法,包括以下步骤:(i)使炔基酰胺环化以形成5-亚甲基恶唑啉(ii)使用三氯氰尿酸酸化5-亚甲基恶唑啉以产生氯化恶唑啉中间体, (iii)用含水酸水解氯代恶唑啉中间体以产生所需的一氯代酮,其中Z是烷基或取代的烷基,芳基或取代的芳基,杂芳基或取代的杂芳基或亚苯基,R是氢原子或烷基,R 1和R 2是 各自独立地是烷基或取代的烷基,或者R 1和R 2与它们所连接的碳原子一起形成环状结构。 此外,当R是氢原子时,可以通过调整反应条件方便地形成二氯酮。