Method for synthesizing N-alkylated indole derivative with high stereoselectivity

The invention belongs to the field of asymmetric catalytic synthesis, and particularly discloses a method for synthesizing an N-alkylated indole derivative with high stereoselectivity. According to the invention, a method for synthesizing the N-alkylindole derivative with high enantioselectivity by...

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Hauptverfasser: SUN JIANGTAO, PENG QUANXIN, SHAO YING, TANG SHENGBIAO
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the field of asymmetric catalytic synthesis, and particularly discloses a method for synthesizing an N-alkylated indole derivative with high stereoselectivity. According to the invention, a method for synthesizing the N-alkylindole derivative with high enantioselectivity by combining a racemic rhodium salt catalyst with a 3-isopropyl indole derivative and aryl or alkyl diazonium ester which are synergistically catalyzed by chiral phosphoric acid is adopted, so that the non-natural amino acid derivative with high stereoselectivity is obtained; the method has the advantages of simple reaction operation, simple and easily available raw materials, mild reaction conditions, wide substrate application range, high efficiency and good enantioselectivity. 本发明属于不对称催化合成领域,具体公开了一种高立体选择性合成N-烷基化吲哚衍生物的方法,本发明采用了消旋铑盐催化剂结合手性磷酸协同催化的3-异丙基吲哚衍生物和芳基或烷基重氮酯高对映选择性合成N-烷基吲哚衍生物的方法,得到了具有高立体选择性的非天然氨基酸衍生物,本发明方法的优点有:反应操作简单、原料简单易得、反应条件温和、底物适用范围广、效率高、对映选择性好。