公开(公告)号：US5681959A

公开(公告)日：1997-10-28

申请号：US604133

申请日：1996-02-20

申请人： Brian Cchristopher Bishop ,  Ian Frank Cottrell ,  Mark Cameron ,  David Hands

发明人： Brian Cchristopher Bishop ,  Ian Frank Cottrell ,  Mark Cameron ,  David Hands

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to a process for the preparation of azaindole derivatives of the formula ##STR1## wherein Q is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-6 alkoxy, hydroxy, aryl or arylC.sub.1-4 alkyl; one of X, Y and Z is --N.dbd. and the others are --CH.dbd.; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.1-6 alkyl substituted by a group selected from aryl or --NR.sup.2 R.sup.3 where R.sup.2 and R.sup.3 each independently represent C.sub.1-4 alkyl, or R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, form a 4-7 membered saturated heterocyclic ring, optionally containing in the ring an oxygen or sulphur atom or a group NR.sup.4 where R.sup.4 is C.sub.1-4 alkyl, aryl or arylC.sub.1-4 alkyl; and R.sup.5 is a hydrogen atom or a group selected from C.sub.1-6 alkyl or aryl.

摘要翻译： 本发明涉及制备式（III）的氮杂吲哚衍生物的方法，其中Q是氢，C 1-6烷基，C 2-6烯基，C 1-6烷氧基，羟基，芳基或芳基C 1-4烷基; X，Y和Z之一为-N =，其余为-CH =; R 1是氢，C 1-6烷基，C 2-6烯基或被选自芳基或-NR 2 R 3的基团取代的C 1-6烷基，其中R 2和R 3各自独立地代表C 1-4烷基，或R 2和R 3与它们所在的氮原子一起 形成4-7元饱和杂环，任选地在环中含有氧或硫原子或基团NR4，其中R4是C1-4烷基，芳基或芳基C1-4烷基; R5为氢原子或选自C1-6烷基或芳基的基团。