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. Author manuscript; available in PMC: 2014 Jun 1.
Published in final edited form as: Chem Sci. 2013 Mar 18;4(6):2374–2379. doi: 10.1039/C3SC50184A

Table 1.

Discovery of C-3 C-H arylation of indazolea

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entry PhI (equiv) ligand base 2a (%)b 3 (%)b
1 1.0 Phen Cs2CO3 24 3
2 2.0 Phen Cs2CO3 51 14
3 2.0 Phen-PhMe Cs2CO3 21 0
4 2.0 Dpya Cs2CO3 42 0
5 2.0 Phen K3PO4 47 6
6 2.0 Phen K2HPO4 3 0
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Phen
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Phen-PhMe
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Dpya
a

Reaction conditions: Indazole (0.25 mmol) in solvent (1 mL) at 140 °C for 48 h.

b

Yield was determined by 1H NMR using CH2Br2 as an internal standard.