Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Cyclopropylamine | HCID 69828 | — |
| Reactant | HCID 69299470 | HCID 69299470 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | HCID 69299514 | HCID 69299514 | 64% |
Reaction Steps
Using general method E, 1-(1-tert-butyl-1H-pyrazol-4-yl)-3-(2-fluoro-4-methyl-5-(8-methyl-2-(methylsulfinyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)urea from Example 109 (0.081 g, 0.16 mmol) and cyclopropanamine (0.027 g, 0.48 mmol) were combined in THF (1 mL) to provide 1-(1-tert-butyl-1H-pyrazol-4-yl)-3-(5-(2-(cyclopropylamino)-8-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)-2-fluoro-4-methylphenyl)urea as a white solid (0.051 g, 64% yield). 1H NMR (400 MHz, DMSO-d6): δ 8.64 (s, 1H), 8.60 (brs, 1H), 8.40 (d, J=1.6 Hz, 1H), 8.06-8.04 (m, 1H), 7.94 (d, J=8.8 Hz, 1H), 7.77 (s, 1H), 7.66 (s, 1H), 7.36 (s, 1H), 7.10 (d, J=12.4 Hz, 1H), 3.61-3.54 (m, 3H), 2.78-2.83 (m, 1H), 2.05 (s, 3H), 1.45 (s, 9H), 0.725 (brs, 2H), 0.55-0.53 (m, 2H); (ESI) m/z: 505.2 (M+H+).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08188113B2 |
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| Source dataset | uspto-grants-2012_05 |
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| ORD ID | ord-18f981cbc4354afb8ae3bcaf89d76f49 |
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| Source note | uspto-grants-2012_05 |
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