Four-Component Synthesis of Fully Substituted 1,2,4-Triazoles

被引:90
作者
Staben, Steven T. [1 ]
Blaquiere, Nicole [1 ]
机构
[1] Genentech Inc, Discovery Chem Grp, San Francisco, CA 94080 USA
关键词
carbonylation; C-C coupling; homogeneous catalysis; multicomponent reactions; nitrogen heterocycles; CROSS-COUPLING REACTIONS; COPPER-CATALYZED ARYLATION; CARBON-MONOXIDE; BORONIC ACIDS; PALLADIUM; HETEROCYCLE; ALTERNATIVES; OXADIAZOLES; EFFICIENT; IMINES;
D O I
10.1002/anie.200905897
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
"Chemical Equation Presented" All 4 one: Palladium-catalyzed carbonylation initiates a highly regioselective triazole synthesis. In this four-partner protocol, the aryl halide, amidine, and hydrazine partners are easily varied, allowing the synthesis of fully substituted 1,2,4-triazoles in a modular fashion. This methodology is demonstrated with the synthesis of druglike and/or pharmaceutically relevant molecules such as deferasirox. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:325 / 328
页数:4
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