7-fluoro-5-nitro-1H-indole synthesis
- Product Name:7-fluoro-5-nitro-1H-indole
- CAS Number:1167055-33-5
- Molecular formula:C8H5FN2O2
- Molecular Weight:180.14
1268816-57-4
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Yield:1167055-33-5 84%
Reaction Conditions:
palladium 10% on activated carbon in xylene; for 2 h;Reflux;
Steps:
39.1
[Example 39] tert-Butyl 4-[2-(7-fluoro-5-nitroindol-1-ylmethyl)pyridin-5-yl]piperidine-1-carboxylate (1) 7-Fluoro-5-nitroindole To a solution of 7-fluoro-5-nitroindoline (Example 36 (1)) (100 mg, 0.55 mmol) in xylene (5 mL) was added 10% palladium-carbon (292 mg, 0.27 mmol) and then the mixture was refluxed for 2 hours. After cooling to room temperature, the insoluble materials were filtered off, and the solvent was removed under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate/hexane = 1/1), to give the title compound as a yellow crystal (83 mg, yield 84%) . 1H NMR (CDCl3 400 MHz): δ= 6.81 (1H, dd, J = 3 Hz, 5 Hz), 7.41(1H, t, J = 3 Hz), 7.86 (1H, dd, J = 2 Hz, 12 Hz), 8.46 (1H, d, J = 2 Hz), 8.5-8.9 (1H, br s).
References:
EP2474540,2012,A1 Location in patent:Page/Page column 41
769966-04-3
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387-44-0
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$24.00/1g
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