A Divergent Approach to the Synthesis of 3-Substituted-2-pyrazolines: Suzuki Cross-Coupling of 3-Sulfonyloxy-2-pyrazolines

被引:18
|
作者
Grimm, Jonathan B. [1 ]
Wilson, Kevin J. [1 ]
Witter, David J. [1 ]
机构
[1] Merck Res Labs, Dept Chem, Boston, MA 02115 USA
来源
JOURNAL OF ORGANIC CHEMISTRY | 2009年 / 74卷 / 16期
关键词
IMIDOYL CHLORIDES; ARYL; DERIVATIVES; ACIDS; CATALYSTS; DESIGN; SCOPE; MILD;
D O I
10.1021/jo9011859
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The efficient Suzuki cross-coupling of pyrazoline nonaflates with organoboron reagents was achieved to afford diverse 3-substituted-2-pyrazolines in excellent yield. The nonaflates displayed improved reactivity over the corresponding triflates and smoothly coupled to a variety of aryl- and heteroarylboronic acids. This process and its broad scope constitute a rapid, divergent strategy for the synthesis of elaborated 2-pyrazolines that are not readily obtained via conventional methods.
引用
收藏
页码:6390 / 6393
页数:4
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