Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Diisopropylethylamine | HCID 81531 | — |
| Reactant | 2,5-Dichloro-N-(5-methyl-1H-pyrazol-3-yl)-4-pyrimidinamine | HCID 11402272 | — |
| Reactant | (S)-1-(5-Fluoropyrimidin-2-yl)ethanamine hydrochloride | HCID 66624037 | — |
| Solvent | 1-Butanol | HCID 263 | — |
| Product | Azd-1480 | HCID 16659841 | 57.3% |
Reaction Steps
A mixture of (5)-1-(5-fluoropyrimidin-2-yl)ethanamine hydrochloride (Method 7, 80 mg), 2,5-dichloro-N-(5-methyl-1H-pyrazol-3-yl)pyrimidin-4-amine (Method 9, 122 mg) and DIPEA (0.134 ml) in n-BuOH (2.5 ml) was charged into a microwave reaction vessel. The vessel was sealed and heated in microwave reactor at 180° C. for 6 hours. The solvent was removed under reduced pressure and the residue was purified by Gilson (10-50% MeCN/H2O, 15 min) to give the titled compound as solid (90 mg). NMR 10.34 (s, 1H), 8.91 (s, 3H), 8.30 (s, 1H), 5.94 (s, 1H), 4.96-5.34 (m, 1H), 2.25 (s, 3H), 1.56 (d, 3H); m/z 350.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08088784B2 |
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| Source dataset | uspto-grants-2012_01 |
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| ORD ID | ord-fd2a37867f3f4dda9343db6628b04a5f |
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| Source note | uspto-grants-2012_01 |
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