6-PIPERAZINYL-3,4-DIHYDROQUINAZOLIN-2(1H)-ONES
    9.
    发明申请
    6-PIPERAZINYL-3,4-DIHYDROQUINAZOLIN-2(1H)-ONES 审中-公开
    6-PIPERAZINYL-3,4-二氢喹唑啉-2(1H) - 酮

    公开(公告)号:US20150374695A1

    公开(公告)日:2015-12-31

    申请号:US14848058

    申请日:2015-09-08

    Inventor: Nisar ULLAH

    CPC classification number: A61K31/517 A01N43/54 C07D239/80 C07D401/12

    Abstract: A series of new 6-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones have been synthesized. The compounds are structurally related to adoprazine, a potential atypical antipsychotics bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling of suitably modified aryl bromides with tert-butyl piperazine-1-carboxylate afforded the advanced intermediate piperazinyl-3,4-dihydroquinazolin-2(1H)-one. The reductive amination of the latter with appropriately designed biarylaldehydes accomplished the synthesis of these compounds.

    Abstract translation: 已经合成了一系列新的6-哌嗪基-3,4-二氢喹唑啉-2(1H) - 酮。 这些化合物在结构上与具有强力D2受体拮抗剂和5-HT1A受体激动剂特性的潜在非典型抗精神病药的阿扑
    肼有关。 适当改性的芳基溴与哌嗪-1-羧酸叔丁酯的Buchwald-Hartwig偶联得到高级中间体哌嗪基-3,4-二氢喹唑啉-2(1H) - 酮。 后者与适当设计的二芳基醛的还原胺化完成了这些化合物的合成。

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