3
1
3. Rice, K. C.; Boone, B. J.; Rubin, A. B.; Rauls, T. J. J. Med. Chem.
976, 19, 887.
14. Gassman P. G.; CueJr. B. W.; Luh, T. Y. J. Org. Chem. 1977, 42, 1344.
O
1
2 5
I O ( 2 equiv.)
O
N
DMSO, 80
0 min
o
C
N
1
5. Stollé, R.; Bergdoll, R.; Luther, M.; Auerhahn, A.; Wacker, W. J. Prakt.
Chem. 1930, 128, 1.
2
1
.6 mmol, 1.000 g
n
2n
6.3 mmol, 1.107 g
7
16. (a) Chaudhari, D. A.; Fernandes, R. A. J. Org. Chem. 2016, 81, 2113; (b)
Wang, H.; Cheng, Y.; Becker, P.; Raabe, G.; Bolm, C. .Angew. Chem. Int.
Ed .2016, 55, 12655.
Scheme 5. Gram-scale experiment
1
7. Matassini, C.; Parmeggiani, C.; Cardona, F.; Goti, A. Org. Lett. 2015, 17,
082.
4
In summary, we have successfully developed a facile protocol
for the direct synthesis of isatins from commercially available
18. Yoshimura, A.; Zhdankin, V. V. Chem. Rev. 2016, 116, 3328.
19. Zi, Y.; Cai, Z.-J.; Wang, S.-Y.; Ji, S.-J. Org. Lett. 2014, 16, 3094.
2
0. Liu, P. J.; Guo, J. J.; Wei, W. T.; Liu, X. Z.; Sun, P. H. Eur. J. Org.
Chem. 2016, 2105.
1. Prathima, P. S.; Bikshapathi, R.; Rao, V. J. Tetrahedron Lett. 2015, 56,
2 5
indoles by using inorganic hypervalent I O as oxidant. The
reaction tolerated a wide variety of functional groups and diverse
isatins were efficiently synthesized in good yields. Notable
features of this method involve high activities, wide substrate
scope and non-toxic oxidant. Further explorations on the
mechanism and extension of this strategy to synthesize other
indole derivatives are ongoing in our laboratory.
2
6
385.
Acknowledgments
We thank the financial support from the National Natural Science
Foundation of China (51578224) and the Natural Science
Foundation of Hunan Province (2015JJ4018).
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