2(1H)-吡嗪酮骨架的固相合成：一种构建多样取代杂环化合物的新方法。

Solid-phase synthesis of the 2(1H)-pyrazinone scaffold: a new approach toward diversely substituted heterocycles.

作者信息

Kaval Nadya, Dehaen Wim, Van der Eycken Erik

机构信息

Laboratory for Organic Synthesis, Department of Chemistry, University of Leuven, Celestijnenlaan 200F, B-3001 Leuven, Belgium.

出版信息

J Comb Chem. 2005 Jan-Feb;7(1):90-5. doi: 10.1021/cc049882e.

DOI:10.1021/cc049882e

PMID:15638486

Abstract

The first solid-phase synthesis of the 2(1H)-pyrazinone scaffold is described. The diversity at position C6 of the pyrazinone ring is determined by the choice of the starting aldehyde. Microwave-enhanced transition metal-catalyzed reactions allow easy introduction of a variety of substituents at the C3 position. This opens a way for the generation of libraries of diversely substituted 2(1H)-pyrazinones that will be screened for biological activities.

摘要

描述了2(1H)-吡嗪酮骨架的首次固相合成。吡嗪酮环C6位的多样性由起始醛的选择决定。微波增强的过渡金属催化反应使得能够在C3位轻松引入各种取代基。这为生成各种取代的2(1H)-吡嗪酮库开辟了道路，这些库将进行生物活性筛选。