Cyclization process for making oxazolikinones
    2.
    发明授权
    Cyclization process for making oxazolikinones 失效
    制备恶唑酮的环化方法

    公开(公告)号:US5688962A

    公开(公告)日:1997-11-18

    申请号:US649843

    申请日:1996-05-16

    CPC分类号: C07D263/18 C07D263/28

    摘要: A process for the synthesis of a compound of general formula II: ##STR1## wherein: R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl; A is an aromatic or heteroaromatic ring system optionally substituted with one or more substituents as defined herein; and in which any ring nitrogen atom may be quaternised or oxidised; alternatively, any two substituents of the group A may combine to form a fused 5- or 6-membered saturated or partially saturated carbocyclic or heterocyclic ring in which any carbon or quaternised nitrogen atom may be substituted with any of the groups defined herein for A or in which a ring carbon atom may be oxidised; the process comprising cyclising a compound of general formula VII: ##STR2## wherein A, R.sup.2 and R.sup.3 are as defined for general formula II, R.sup.20 is hydrogen, benzyl or benzyl substituted with up to five substituents selected from halo, C.sub.1 -C.sub.6 alkyl, O(C.sub.1 -C.sub.6 alkyl) or nitro and R.sub.21 is C.sub.1 -C.sub.8 alkyl, benzyl or benzyl substituted with up to five of the substituents mentioned above for R.sup.20.

    摘要翻译: 合成通式II化合物的方法:其中:R 2和R 3各自独立地为氢或C 1 -C 4烷基; A是任选被一个或多个如本文定义的取代基取代的芳族或杂芳族环系统; 并且其中任何环氮原子可被季铵化或氧化; 可选地,基团A的任何两个取代基可以结合形成稠合的5-或6-元饱和或部分饱和的碳环或杂环,其中任何碳或季铵化的氮原子可以被本文定义的任何A或 其中环碳原子可被氧化; 该方法包括环化通式VII的化合物:其中A,R 2和R 3如通式II所定义,R 20是氢,被至多5个选自卤素,C 1 -C 6烷基的取代基取代的苄基或苄基 ,O(C 1 -C 6烷基)或硝基,R 21是C 1 -C 8烷基,被至多5个上述R 20取代基取代的苄基或苄基。