Abstract

The electrophilic reactivity of a series of novel pyrazole-4,5-dione derivatives in the organocatalytic Friedel–Crafts reaction with various substituted indoles has been tested. The disclosed procedure catalyzed by a cinchona alkaloid derivative allows the conjugation of two very important aza-heterocyclic scaffolds to generate a new class of indolylpyrazolones bearing a tetrasubstituted stereocenter in excellent yields (up to 99%) and with enantioselectivities of up to 94:6 er.

The electrophilic reactivity of a series of novel pyrazole-4,5-dione derivatives in the organocatalytic Friedel–Crafts reaction with various substituted indoles has been tested. The disclosed procedure catalyzed by a cinchona alkaloid derivative allows the conjugation of two very important aza-heterocyclic scaffolds to generate a new class of indolylpyrazolones bearing a tetrasubstituted stereocenter in excellent yields (up to 99%) and with enantioselectivities of up to 94:6 er.

中文翻译：

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使用不对称吡唑-4,5-二酮类化合物的不对称有机催化弗里德-克拉夫茨对吲哚的羟烷基化反应

摘要

测试了一系列新型吡唑-4,5-二酮衍生物在有机催化的Friedel-Crafts反应中与各种取代的吲哚的亲电反应性。由金鸡纳生物碱衍生物催化的所公开的方法允许两个非常重要的氮杂杂环支架的缀合以优异的产率（高达99％）和对映选择性高达94：6 er产生带有四取代的立体中心的新型吲哚并吡唑啉酮。 。

测试了一系列新型吡唑-4,5-二酮衍生物在有机催化的Friedel-Crafts反应中与各种取代的吲哚的亲电反应性。由金鸡纳生物碱衍生物催化的所公开的方法允许两个非常重要的氮杂杂环支架的缀合以优异的产率（高达99％）和对映选择性高达94：6 er产生带有四取代的立体中心的新型吲哚并吡唑啉酮。 。