Journal
ORGANIC LETTERS
Volume 15, Issue 20, Pages 5270-5273Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol402494e
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Funding
- NSFC [21072079, 21272100]
- Program for New Century Excellent Talents in University [NCET-11-0215]
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The first Pd(II)-catalyzed C-H addition to isatins by direct sp(2)/sp(3) C-H bond activation for the construction of 3-substituted-3-hydroxy-2-oxindoles is reported. The bidentate nitrogen ligands were found to promote this reaction. Specifically, the preliminary bioassay indicated that 3-(5-chlorobenzoxazole)-3-hydroxy-N-benzyl-2-oxindole (2w) is a new inhibitor of human kidney cancer and hepatocellular carcinoma cells. Moreover, this reaction system exhibits great functional group tolerance and requires no directing group, extra base, or additives.
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