Process for the preparation of C(5)-substituted
1,2-dihydro-5H-chromeno[3,4-f] quinolines
    15.
    发明授权
    Process for the preparation of C(5)-substituted 1,2-dihydro-5H-chromeno[3,4-f] quinolines 失效
    制备C(5) - 取代的1,2-二氢-5H-色烯并[3,4-f]喹啉的方法

    公开(公告)号:US6093826A

    公开(公告)日:2000-07-25

    申请号:US93421

    申请日:1998-06-08

    CPC classification number: C07D491/04

    Abstract: A method for preparing C(5)-substituted 1,2-dihydro-5H-chromeno[3,4-.function.]quinolines from a lactol precursor is provided. The method comprises converting the lactol to one of a select number of mixed acetal derivatives, and then treating the acetals with a Grignard reagent. The new process provides products in higher yield and greater purity. Novel intermediates of this method are also claimed.

    Abstract translation: 提供了从乳糖前体制备C(5) - 取代的1,2-二氢-5H-色烯并[3,4-f]喹啉的方法。 该方法包括将乳糖转化为选定数量的混合缩醛衍生物之一,然后用格氏试剂处理该缩醛。 新工艺提供了更高产量和更高纯度的产品。 还要求保护该方法的新型中间体。

    Methods for preparation of 1,2-dihydroquinolines
    16.
    发明授权
    Methods for preparation of 1,2-dihydroquinolines 失效
    1,2-二氢喹啉的制备方法

    公开(公告)号:US6093825A

    公开(公告)日:2000-07-25

    申请号:US86004

    申请日:1998-05-27

    CPC classification number: C07D491/04

    Abstract: Methods for conversion of anilines to 1,2-dihydroquinolines. 1,2-dihydroquinoliiies are generated from combining an aniline, a silylating agent, and further condensing with a ketone in the presence of a catalyst. In one aspect, the silylation of the aniline may be performed in a one-step synthesis by adding the silylating, agent to the same reaction vessel as the ketone, aniline, and catalyst. In a second aspect, the 1,2-dihydroquinoline is generated in a two-step synthesis where an N-silyl aniline is formed prior to the addition of the ketone and catalyst.

    Abstract translation: 将苯胺转化为1,2-二氢喹啉的方法。 1,2-二氢喹啉由苯胺,甲硅烷化剂组合,并在催化剂存在下与酮进一步缩合而产生。 一方面,苯胺的甲硅烷基化可以通过将甲硅烷基化试剂加入到与酮,苯胺和催化剂相同的反应容器中,在一步合成中进行。 在第二方面,1,2-二氢喹啉是在加入酮和催化剂之前形成N-甲硅烷基苯胺的两步合成中产生的。

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