Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Sodium Carbonate | HCID 10340 | — |
| Edukt | 1,2,4-Trifluoro-5-(methylsulfonyl)benzene | HCID 46739396 | — |
| Edukt | HCID 67470730 | HCID 67470730 | — |
| Lösungsmittel | Dimethylformamide | HCID 6228 | — |
| Produkt | HCID 86688112 | HCID 86688112 | 28% |
Reaktionsschritte
(S)-1′-(5-ethylpyrimidin-2-yl)-3-(methylamino)-1,4′-bipiperidin-2-one (0.040 g, 0.13 mmol), 1,2,4-trifluoro-5-(methylsulfonyl)benzene (Preparation C, 0.053 g, 0.25 mmol) and Na2CO3 (0.040 g, 0.38 mmol) were dissolved in DMF (1 mL) and heated at 130° C. overnight. The reaction was concentrated and the residue was purified using preparative TLC (100% EtOAc) to afford (S)-3-((2,5-difluoro-4-(methylsulfonyl)phenyl)(methyl)amino)-1′-(5-ethylpyrimidin-2-yl)-1,4′-bipiperidin-2-one (0.018 g, 0.035 mmol, 28% yield) as yellow solid. Mass spectrum (apci) m/z=508.3 (M+H).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patentnummer | US08754226B2 |
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| Quelldatensatz | uspto-grants-2014_06 |
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| ORD ID | ord-e88004b53ccb4100a1ec2b880703e257 |
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| Quellennotiz | uspto-grants-2014_06 |
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