Journal
ORGANIC LETTERS
Volume 20, Issue 20, Pages 6530-6533Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.8b02856
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Funding
- Strategic Priority Research Program of the Chinese Academy of Sciences [XDB20000000]
- National Basic Research Program of China (973 Program) [2015CB856600]
- National Science Foundation of China [21602213, 21522208, 21372209]
- China Postdoctoral Science Foundation [2017M622255]
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A palladium-catalyzed, amine-directed C(sp(2))-H carbonylation of alpha,alpha-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.
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