Synthesis method of 2-aryl benzazepine and derivatives thereof

The invention relates to a synthesis method of 2-aryl benzazepine and derivatives thereof, the method comprises the following steps: stirring and reacting 2-halogenated aniline and aryl cyclobutanol as reaction substrates, palladium chloride as a catalyst, tricyclohexylphosphine as a ligand, cesium...

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Hauptverfasser: ZHANG XINGGUO, ZENG MENGQIANG, ZHANG XIAOHONG, TU HAIYONG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to a synthesis method of 2-aryl benzazepine and derivatives thereof, the method comprises the following steps: stirring and reacting 2-halogenated aniline and aryl cyclobutanol as reaction substrates, palladium chloride as a catalyst, tricyclohexylphosphine as a ligand, cesium carbonate as alkali and ultra-dry toluene as a solvent in a nitrogen atmosphere at 110 DEG C for 12 hours. The method has the advantages of simple and easily available raw materials, relatively mild reaction conditions, wide substrate universality, novel preparation process, low energy consumption and the like. 本发明涉及一种2-芳基苯并氮杂卓及其衍生物的合成方法,包括以下步骤:以2-卤代苯胺和芳基环丁醇为反应底物,以氯化钯为催化剂,三环己基膦为配体,碳酸铯作碱,超干甲苯作溶剂,于110 oC在氮气氛围中搅拌反应12小时。该方法具有原料简单易得、反应条件相对温和、底物普适性广,制备工艺新颖、耗能低等优点。