Two-step synthesis of β-alkyl chalcones and their use in the synthesis of 3,5-diaryl-5-alkyl-4,5-dihydropyrazoles

被引：32

作者：

Cox, CD ^{[1
]}

Breslin, MJ ^{[1
]}

Mariano, BJ ^{[1
]}

机构：

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

来源：

TETRAHEDRON LETTERS | 2004年 / 45卷 / 07期

关键词：

alkyl chalcone; dihydropyrazole; cyclization; aryl cuprate addition; propargylic ketone;

D O I：

10.1016/j.tetlet.2003.12.026

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

We report a simple and efficient two-step synthesis of variously substituted beta-alkyl chalcones (7) from the corresponding Weinreb amide and a terminal alkyne, and that these chalcones are useful intermediates for the synthesis of medicinally interesting 3,5-diaryl-5-alkyl-4,5-dihydropyrazoles (6). The current methodology allows for the incorporation of many substitution patterns not available from the few previously reported approaches to compounds in this class. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：1489 / 1493

页数：5

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