Ligand-Promoted C(sp(3) )-H Olefination en Route to Multi-functionalized Pyrazoles.
Ligand-Promoted C(sp(3) )-H Olefination en Route to Multi-functionalized Pyrazoles.
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DOI：
10.1002/chem.201600704
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发表时间：
2016-05-17
期刊：
影响因子：
--
通讯作者：
Yu JQ
中科院分区：
文献类型：
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作者：
Yang W;Ye S;Schmidt Y;Stamos D;Yu JQ
发展了Pd催化的/N-杂环导向的C（sp3）-H烯化反应。首次发现单保护氨基酸配体（MPAA）对Pd催化的C（sp3）-H烯化反应有显著的促进作用。Cu（OAc）2代替Ag+盐用作末端氧化剂。该反应为烷基化吡唑类化合物的合成提供了一种有效的方法。研究了吡唑导向的C（sp3）-H烯化反应。首次发现单保护氨基酸配体（MPAA）对Pd催化的C（sp3）-H烯化反应有显著的促进作用。证明了使用该反应用于吡唑基复合物支架的后期多样化的适用性。
A Pd-catalyzed/N-heterocycle-directed C(sp3)–H olefination has been developed. The monoprotected amino acid ligand (MPAA) is found to significantly promote Pd-catalyzed C(sp3)–H olefination for the first time. Cu(OAc)2 instead of Ag+ salts are used as the terminal oxidant. This reaction provides a useful method for the synthesis of alkylated pyrazoles. A pyrazole-directed C(sp3)–H olefination has been developed. The monoprotected amino acid ligands (MPAA) are found to significantly promote the reactivity in Pd-catalyzed C(sp3)–H olefination for the first time. The applicability of using this reaction for late-stage diversification of pyrazole-based complex scaffold are demonstrated.