Journal
ORGANIC LETTERS
Volume 21, Issue 14, Pages 5694-5698Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b02037
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Funding
- Zhejiang Natural Science Fund for Young Scholars [LQ18B020008]
- Zhejiang Sci-Tech University [17062078-Y]
- National Natural Science Foundation of China [21772177]
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A cobalt-catalyzed C-H carbonylation of naphthylamides for the synthesis of benzo[cd]indol-2(1H)-one scaffolds has been developed. The reaction employs a traceless directing group and uses benzene-1,3,5-triyltriormate as the CO source, affording various free (NH)-benzo[cd]indol-2(1H)-ones in moderate to high yields (up to 88%). Using this protocol, the total synthesis of BET bromodomain inhibitors A and B was accomplished as well.
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