Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Sodium Carbonate | HCID 10340 | — |
| Edukt | 4-Bromo-2,5-difluorobenzenesulfonamide | HCID 2773293 | — |
| Edukt | (1S,2R)-4-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)benzeneboronic acid | HCID 54413593 | — |
| Katalysator | HCID 178418397 | HCID 178418397 | — |
| Lösungsmittel | Ethanol | HCID 702 | — |
| Produkt | HCID 57221958 | HCID 57221958 | 36,9% |
Reaktionsschritte
Prepared according to the method described in Example 12) from (1S,2R)-4-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)benzeneboronic acid (0.2 g, Example 33), 4-bromo-2,5-difluorobenzenesulfonamide (0.19 g, Example 37a)), ethanol (3 ml), 2M aqueous sodium carbonate (0.7 ml) and tetrakis(triphenylphosphine)palladium (0) (0.03 g) with heating at 80° C. for 3 hours. After work-up, the residue was purified by normal-phase HPLC eluting with a gradient of 0-25% ethanol in dichloromethane to give the title compound as a foam (0.11 g).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patentnummer | US06300352B1 |
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| Quelldatensatz | uspto-grants-2001_10 |
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| ORD ID | ord-40aa2691177f42fb8a7f311de55bd7c5 |
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| Quellennotiz | uspto-grants-2001_10 |
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