一种温和且高效的4-喹诺酮和喹诺酮杂环化合物的合成方法。

A mild and efficient synthesis of 4-quinolones and quinolone heterocycles.

作者信息

Zewge Daniel, Chen Cheng-Yi, Deer Curtis, Dormer Peter G, Hughes Dave L

机构信息

Department of Process Research, Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA.

出版信息

J Org Chem. 2007 May 25;72(11):4276-9. doi: 10.1021/jo070181o. Epub 2007 Apr 26.

DOI:10.1021/jo070181o

PMID:17458997

Abstract

The cycloacylation of aniline derivatives to 4-quinolones in the presence of Eaton's reagent is described. This high-yielding methodology is applicable to a wide variety of functionalized anilines and requires milder conditions than those traditionally employed. This cyclization protocol is used to prepare a host of heterocycles and bis-quinolones and is characterized by relatively low reaction temperature and ease of product isolation.

摘要

本文描述了在伊顿试剂存在下，苯胺衍生物环酰化生成4-喹诺酮的反应。这种高产率方法适用于多种功能化苯胺，且所需条件比传统方法更为温和。该环化反应方案用于制备一系列杂环化合物和双喹诺酮，其特点是反应温度相对较低且产物易于分离。