Synthesis of β-Keto Esters In-Flow and Rapid Access to Substituted Pyrimidines

被引：37

作者：

Bartrum, Hannah E. ^{[1
]}

Blakemore, David C. ^{[2
]}

Moody, Christopher J. ^{[1
]}

Hayes, Christopher J. ^{[1
]}

机构：

[1] Univ Nottingham, Sch Chem, Nottingham NG7 2RD, England

[2] Pfizer Global Res & Dev, Sandwich CT13 9NJ, Kent, England

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2010年 / 75卷 / 24期

基金：

英国工程与自然科学研究理事会;

关键词：

C-H INSERTION; ETHYL DIAZOACETATE; MULTISTEP SYNTHESIS; CATALYZED SYNTHESIS; AROMATIC-ALDEHYDES; ALPHA-DIAZOESTERS; TIN(II) CHLORIDE; DERIVATIVES; ACID; CONDENSATION;

D O I：

10.1021/jo101783m

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

We have developed an in-flow process for the synthesis of beta-keto esters via the BF3 center dot OEt2-catalyzed formal C-H insertion of ethyl diazoacetate into aldehydes. The beta-keto esters were then condensed with a range of amidines to give a variety of 2,6-substituted pyrimidin-4-ols.

引用

页码：8674 / 8676

页数：3

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