在流相中合成β-酮酯和快速获得取代嘧啶。

Synthesis of β-keto esters in-flow and rapid access to substituted pyrimidines.

机构信息

School of Chemistry, University of Nottingham, University Park, Nottingham, NG7 2RD, United Kingdom.

出版信息

J Org Chem. 2010 Dec 17;75(24):8674-6. doi: 10.1021/jo101783m. Epub 2010 Nov 17.

Abstract

We have developed an in-flow process for the synthesis of β-keto esters via the BF(3)·OEt(2)-catalyzed formal C-H insertion of ethyl diazoacetate into aldehydes. The β-keto esters were then condensed with a range of amidines to give a variety of 2,6-substituted pyrimidin-4-ols.

摘要

我们开发了一种在流动过程中通过 BF(3)·OEt(2)催化的乙基重氮乙酸酯对醛的形式 C-H 插入合成β-酮酯的方法。然后，β-酮酯与一系列脒缩合，得到各种 2,6-取代的嘧啶-4-醇。