Preparation method of isoxazole six-membered heterocyclic derivative

The invention discloses a preparation method of an isoxazolo six-membered heterocyclic derivative, which comprises the following steps: adding raw materials including a 4-benzylidene-3-phenylisoxazole-5-ketone compound, acetonitrile, dichloromethane, olefin and boron trifluoride diethyl etherate int...

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Hauptverfasser: QIAN SHENCHENG, ZHENG YU, HUANG SHENLIN, MA TIANTING
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a preparation method of an isoxazolo six-membered heterocyclic derivative, which comprises the following steps: adding raw materials including a 4-benzylidene-3-phenylisoxazole-5-ketone compound, acetonitrile, dichloromethane, olefin and boron trifluoride diethyl etherate into a reaction flask, and stirring for 5 hours at the temperature of 40 DEG C at the speed of 300-600rpm. And after the reaction is finished, concentrating the reaction liquid, and performing column chromatography separation to obtain a target product. The whole reaction successfully avoids the use of a metal catalyst, the raw materials required by the reaction are cheap, the reaction conditions are mild, the operation is simple and convenient, and the product has a good application prospect. 本发明公开了一种异噁唑并六元杂环衍生物的制备方法,其包括,将原料4-苄叉-3-苯基异噁唑-5-酮类化合物、乙腈、二氯甲烷、烯烃和三氟化硼乙醚加入反应瓶中,以300~600rpm在40℃下搅拌5h。反应结束后,浓缩反应液,再经柱层析分离得到目标产物。整个反应成功避免了金属催化剂的使用,反应所需原料廉价,反应条件温和、操作简便,产品具有很好的应用前景。