Total Synthesis of Natural Product Piperodione and Its Analogues,ChemistrySelect

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Total Synthesis of Natural Product Piperodione and Its Analogues
ChemistrySelect ( IF 1.9 ) Pub Date : 2018-06-04 , DOI: 10.1002/slct.201801427
Praveen Kumar Tiwari ₁ , Hemkalyan Ballav ₁ , Indrapal Singh Aidhen ₁

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Two new approaches for the synthesis of natural product piperodione, secondary metabolite have been achieved. Hitherto, unknown and easily accessible piperidine and morpholine based α‐ketoamide phosphoranes obtained from pyruvic acid have served as key building blocks for synthesis based on Wittig reaction. The alkylation of β‐keto esters with 3‐bromo derivative of pyruvic acid amides has been equally successful. Both the developed routes have enabled access to several new analogues of piperodione, opening up opportunities for systematic structure activity relationships studies during evaluation of biological activity.

中文翻译：

天然产物哌啶酮的全合成及其类似物

已经实现了两种用于合成天然产物哌啶酮，次生代谢物的新方法。迄今为止，从丙酮酸获得的未知且易于获得的哌啶和吗啉基α-酮酰胺膦烷已成为基于Wittig反应合成的关键组成部分。用丙酮酸酰胺的3-溴衍生物将β-酮酯烷基化也同样成功。两条已开发的途径都使人们能够使用几种新的哌啶酮类似物，从而为生物活性评估过程中系统的结构活性关系研究提供了机会。

更新日期：2018-06-04

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