Gold-catalyzed three-component annulation: efficient synthesis of highly functionalized dihydropyrazoles from alkynes, hydrazines, and aldehydes or ketones.
Gold-catalyzed three-component annulation: efficient synthesis of highly functionalized dihydropyrazoles from alkynes, hydrazines, and aldehydes or ketones.
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DOI：
10.1021/ol203072u
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发表时间：
2012-01
期刊：
影响因子：
5.2
通讯作者：
Yamato Suzuki;Saori Naoe;S. Oishi;N. Fujii;H. Ohno
中科院分区：
文献类型：
--
作者：
Yamato Suzuki;Saori Naoe;S. Oishi;N. Fujii;H. Ohno
通过金催化的三组分环合反应直接合成了多取代二氢吡唑。该反应由炔与N，N '-二取代肼和醛/酮的Mannich型偶联，随后是分子内氢胺化组成。使用1，2-二炔基苯衍生物作为炔组分的级联环化反应也以良好的产率进行生产稠合三环二氢吡唑。
Polysubstituted dihydropyrazoles were directly obtained by a gold-catalyzed three-component annulation. This reaction consists of a Mannich-type coupling of alkynes with N,N'-disubstituted hydrazines and aldehydes/ketones followed by intramolecular hydroamination. Cascade cyclization using 1,2-dialkynylbenzene derivatives as the alkyne component was also performed producing fused tricyclic dihydropyrazoles in good yields.