Journal
ORGANIC LETTERS
Volume 15, Issue 17, Pages 4528-4531Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol4020877
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Funding
- National Natural Science Foundation of China [21290180, 20972007]
- National Basic Research Program of China (973 Program) [2010CB833200]
- State Key Laboratory of Drug Research
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The first Pd-catalyzed method for direct olefination at the C4 position of tryptophan derivatives has been developed via C-H activation to prepare 4-substituted tryptophans, which could be used for the synthesis of many hemiterpenoid indole alkaloids. This reaction proceeds under mild reaction conditions and with exceptional tolerance to a variety of functional groups. Furthermore, the efficiency of this method is demonstrated by the rapid and biomimetic synthesis of clavicipitic acid.
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