钯(II)催化一氧化碳与位阻胺的 C(sp)-H 羰基化反应。
Palladium(II)-Catalyzed C(sp)-H Carbonylation of Sterically Hindered Amines with Carbon Monoxide.
机构信息
Hefei National Laboratory for Physical Sciences at the Microscale and Department of Chemistry, Center for Excellence in Molecular Synthesis of CAS , University of Science and Technology of China , 96 Jinzhai Road , Hefei 230026 , China.
College of Chemistry, Chemical Engineering and Material Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Institute of Molecular and Nano Science , Shandong Normal University , Jinan 250014 , China.
出版信息
Org Lett. 2018 Oct 19;20(20):6530-6533. doi: 10.1021/acs.orglett.8b02856. Epub 2018 Oct 9.
A palladium-catalyzed, amine-directed C(sp)-H carbonylation of α,α-disubstituted benzylamine under 1 atm of CO for the facile synthesis of sterically hindered benzolactam has been developed. The key to success is the use of 2,2,6,6-tetramethyl-1-piperidinyloxy as the crucial sole oxidant. The synthetic utility of this transformation has been demonstrated by the first concise synthesis of the natural product spiropachysin-20-one.
发展了一种钯催化、胺导向的α,α-二取代苄胺 C(sp)-H 羰基化反应，在 1 个大气压的 CO 下，可方便地合成空间位阻较大的苯并内酰胺。成功的关键是使用 2,2,6,6-四甲基-1-哌啶醇作为关键的单一氧化剂。该转化的合成实用性已通过天然产物螺帕嗪-20-酮的首次简洁合示。
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