High-throughput synthesis of N3-acylated dihydropyrimidines combining microwave-assisted synthesis and scavenging techniques

被引：138

作者：

Dallinger, D ^{[1
]}

Gorobets, NY ^{[1
]}

Kappe, CO ^{[1
]}

机构：

[1] Karl Franzens Univ Graz, Inst Chem, A-8010 Graz, Austria

来源：

ORGANIC LETTERS | 2003年 / 5卷 / 08期

关键词：

D O I：

10.1021/ol034085v

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The solution-phase synthesis of N3-acylated dihydropyrimidines was achieved utilizing microwave flash heating both in the synthesis (acylation) and purification (scavenging) steps. Quenching times for excess anhydrides using polystyrene or silica-supported diamine sequestration reagents were reduced from several hours to minutes utilizing microwave irradiation. The use of water as sequestration agent, coupled with an efficient solid-phase extraction workup technique allowed the rapid generation of a 20-member library of N3-acylated dihydropyrimidines.

引用

页码：1205 / 1208

页数：4

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