Asymmetric Deoxygenative Alkynylation of Tertiary Amides Enabled by Iridium/Copper Bimetallic Relay Catalysis
Asymmetric Deoxygenative Alkynylation of Tertiary Amides Enabled by Iridium/Copper Bimetallic Relay Catalysis
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DOI：
10.1002/anie.202111029
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发表时间：
2021-11-10
影响因子：
16.6
通讯作者：
Wang, Xiaoming
中科院分区：
文献类型：
--
作者：
Li, Zhaokun;Zhao, Feng;Wang, Xiaoming
通过Ir催化的部分还原反应和Cu/GARPHOS催化的末端炔的不对称炔基化反应，以高产率和良好的对映选择性将多种惰性叔酰胺成功地转化为重要的手性炔丙胺。该反应很容易扩展到一些药物分子，并已证明了代表性产物的转化，从而证明了该方案的实用性和稳健性。
A variety of inert tertiary amides have been successfully transformed into synthetically important chiral propargylamines in high yields with good to excellent enantioselectivities via a relayed sequence of Ir catalyzed partial reduction and Cu/GARPHOS catalyzed asymmetric alkynylation with terminal alkynes. The reaction was readily extended to some drug molecules and the transformations of representative products have been demonstrated, thus attesting the practical utilities and the robust nature of the protocol.