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. Author manuscript; available in PMC: 2018 Jan 1.
Published in final edited form as: J Heterocycl Chem. 2015 Nov 25;54(1):155–160. doi: 10.1002/jhet.2559

Table 1.

Preparation of 3-Aryl and 3-Cyclopropyl Derivatives of 1,2,4-Benzotriazine 1-Oxide.

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Aryl halide R2, product Yield [%] Ligand Base Solvent
3a 4-cyanophenyl, 5 66 SPhos Cs2CO3 Toluene
3b 74 SPhos Cs2CO3 Toluene
3a 4-bromophenyl, 6 trace PCy3 K3PO4 MeCN/Water
3b 57 PCy3 K3PO4 MeCN/Water
3a 4-nitrophenyl, 7 42 SPhos Cs2CO3 Toluene
3b 65 SPhos Cs2CO3 Toluene
3a quinolin-2-yl, 8 29 SPhos K3PO4 Toluene/Water
3b 40 SPhos K3PO4 Toluene/Water
3a cyclopropyl, 9 76 SPhos Cs2CO3 Toluene
3b 80 SPhos Cs2CO3 Toluene
3b 4-N-Boc-aminophenyl, 10 61 SPhos K3PO4 Toluene/Water