HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 59151Erstellt: 23. Oktober 2026
Cesium carbonate → 4-(4,4-Difluoropiperidin-1-yl)-N-(3-methoxy-4-(6-methylpyridazin-4-yl)phenyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-2-amine
https://huagongshe.com/de/reaction/59151
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Cesium carbonate | HCID 10796 | — |
| Edukt | 2-(Dicyclohexylphosphino)biphenyl | HCID 2734216 | — |
| Edukt | 3-Methoxy-4-(6-methylpyridazin-4-yl)aniline | HCID 66859066 | — |
| Edukt | 2-Chloro-4-(4,4-difluoropiperidin-1-yl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine | HCID 117821130 | — |
| Katalysator | palladium(II) acetate | HCID 167845 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | 4-(4,4-Difluoropiperidin-1-yl)-N-(3-methoxy-4-(6-methylpyridazin-4-yl)phenyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-2-amine | HCID 86344804 | — |
Reaktionsschritte
A mixture of 2-chloro-4-(4,4-difluoropiperidin-1-yl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine (40 mg, 0.12 mmol), 3-methoxy-4-(6-methylpyridazin-4-yl)aniline (25 mg, 0.12 mmol), cesium carbonate (75 mg, 0.23 mmol), palladium(II) acetate (4 mg, 0.02 mmol) and 2-(dicyclohexylphosphino)biphenyl (6 mg, 0.02 mmol) in dioxane (2 mL) was heated under argon at 120° C. for 90 minutes in a microwave reactor. The mixture was filtered through a short silica gel plug which was washed with 10% solution of methanol in ethyl acetate (75 mL) and the eluate was concentrated in vacuum. The residue was purified by preparative HPLC to give the title compound as a solid, 35 mg (58%).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patentnummer | US09439904B2 |
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| Quelldatensatz | uspto-grants-2016_09 |
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| ORD ID | ord-d34d6ade3ddc4011a1057bfd59a5a48f |
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| Quellennotiz | uspto-grants-2016_09 |
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