Palladium(II)-Catalyzed Regioselective syn-Hydroarylation of Disubstituted Alkynes Using a Removable Directing Group
Palladium(II)-Catalyzed Regioselective syn-Hydroarylation of Disubstituted Alkynes Using a Removable Directing Group
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DOI：
10.1021/jacs.6b08818
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发表时间：
2016-10-05
影响因子：
15
通讯作者：
Engle, Keary M.
中科院分区：
文献类型：
--
作者：
Liu, Zhen;Derosa, Joseph;Engle, Keary M.
发展了钯(II)催化的高丙醇胺的区域选择性合成氢芳基化反应，其中选择性由可裂解的双齿导向基团控制：在优化的反应条件下，二烷基和烷基芳基都发生了高选择性的氢芳基化反应。该反应的产物含有4，4-二取代的高烯丙基胺基序，这种基序在药物分子和其他生物活性化合物中很常见。
A palladium(II)-catalyzed regioselective syn-hydroarylation reaction of homopropargyl amines has been developed, wherein-selectivity is controlled by a cleavable bidentate directing group: Under the optimized reaction conditions, both dialkyl and alkylaryl substrates were found to undergo hydroarylation with high selectivity. The products of this reaction contain a 4,4-disubstituted homoallylic amine motif that is commonly seen in drug molecules and other bioactive compounds.