Palladium-Catalyzed Cascade Synthesis of Novel Quinolone- Bis(indolyl)methane Hybrids as Promising α-Glucosidase Inhibitors,Synthesis

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Palladium-Catalyzed Cascade Synthesis of Novel Quinolone- Bis(indolyl)methane Hybrids as Promising α-Glucosidase Inhibitors
Synthesis ( IF 2.2 ) Pub Date : 2020-03-30 , DOI: 10.1055/s-0039-1690871
Sheng Liu _{1,

2} , Lian Duan _{1,

2} , Ming-Xing Zuo _{1,

2} , Kai-Qiang Xie _{1,

2} , Yuan-Cui Liu _{1,

2} , Wen-Zhuang Qiu _{1,

2} , Li-Ping Wang _{1,

2}

Affiliation

An unexpected cascade reaction is developed for the construction of functionalized 3-bis(indol-3-yl)methylquinoline-2(1H)-ones. Three C–C bonds and one ring are created in one pot triggered by Pd-catalyzed C-3 alkenylation of indole with 2-acyl-N-acrylaniline derivatives. A series of complex and specific quinoline-2(1H)-ones were produced, most of them showed significant α-glucosidase inhibitory activities.

中文翻译：

钯催化的新型喹诺酮-双（吲哚基）甲烷杂化体作为有希望的α-葡萄糖苷酶抑制剂的级联合成

开发了一种意外的级联反应，用于功能化的3-双（吲哚-3-基）甲基喹啉-2（1 H）-one的构建。在一个锅中，由Pd催化的吲哚与2-酰基-N-丙烯酸苯胺衍生物的C-3烯基化反应会生成三个C–C键和一个环。产生了一系列复杂且特异性的喹啉-2（1 H）-one，其中大多数显示出显着的α-葡萄糖苷酶抑制活性。

更新日期：2020-04-21

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