Efficient synthesis of highly functionalized tetrahydropyridopyrimidines by a novel three-component coupling reaction

被引：3

作者：

Raheem, Izzat T. ^{[1
]}

Schreier, John D. ^{[1
]}

Breslin, Michael J. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA

来源：

TETRAHEDRON LETTERS | 2011年 / 52卷 / 30期

关键词：

Three-component coupling; Tetrahydropyridopyrimidine; Pharmacophore; Reaction optimization;

D O I：

10.1016/j.tetlet.2011.05.071

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

We report the development of a novel three-component coupling reaction (3CC) for the synthesis of alkoxy tetrahydropyridopyrimidines. Systematic optimization of reaction parameters identified 3CC conditions tolerant of a wide array of functionality at all three sites of diversity, providing densely functionalized products in moderate to excellent yields. The newly developed chemistry has since been applied to the lead optimization process on a novel drug discovery program, facilitating rapid compound advancement. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：3849 / 3852

页数：4

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