UPDATES
chromatography (hexane:AcOEt=100:0~85:15) to afford
3aa (169 mg, 88% yield) as a light-yellow solid (mp 119.7–
121.48C).
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1
2
3
4
5
6
7
8
9
2016, 18, 4628–4632.
General procedure for Cadogan cyclization. Synthesis of 2-
(trifluoromethyl)-3-(3,4,5-trimethoxyphenyl)-1H-indole
(4aa): A solution of 3aa (115 mg, 0.30 mmol), MoCl2O2
(dmf)2 (5.18 mg, 0.015 mmol), and PPh3 (195 mg, 0.72 mmol)
in toluene (3.0 mL) was degassed at À788C and then was
stirred at 808C under an argon atmosphere for 3 h. The
reaction mixture was concentrated in vacuo. The residue was
purified by silica gel column chromatography (hexane:
AcOEt=100:0~85:15) to give indole 4aa (102 mg, 97%
yield) as a colorless solid (mp 119.7–120.68C).
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Acknowledgements
This research is partially supported by the Platform Project
for Supporting in Drug Discovery and Life Science Research
from Japan Agency for Medical Research and Development.
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Adv. Synth. Catal. 2017, 359, 1–6
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