Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Phenol | HCID 996 | — |
| Reactant | Potassium Carbonate | HCID 11430 | — |
| Reactant | 4,5-Dichloro-2-(tetrahydro-pyran-2-yl)-2H-pyridazin-3-one | HCID 10729262 | — |
| Solvent | Acetonitrile | HCID 6342 | — |
| Product | HCID 66875343 | HCID 66875343 | 92.3% |
Reaction Steps
A solution of 4,5-dichloro-2-(tetrahydropyran-2-yl)-2H-pyridazin-3-one (Intermediate 20, 2.50 g, 10.03 mmol) in acetonitrile (111 mL, 0.09M) was treated with potassium carbonate (1.38 g, 10.03 mmol) and phenol (944 mg, 10.03 mmol). The resulting reaction mixture was heated at reflux for 3 h and then was allowed to cool to 25° C. The reaction mixture was then partitioned between water (150 mL) and methylene chloride (3×100 mL). The combined organics were dried over sodium sulfate, filtered, rinsed, and concentrated in vacuo. Silica gel column chromatography (ISCO 80 g, 30% ethyl acetate/hexanes) afforded 4-chloro-5-phenoxy-2-(tetrahydro-pyran-2-yl)-2H-pyridazin-3-one (2.84 g, 92%) as a clear oil; ES+-HRMS m/e calcd for C15H15N2O3Cl [M+H+] 307.0844, found 307.0843.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08258134B2 |
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| Source dataset | uspto-grants-2012_09 |
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| ORD ID | ord-98fabfbfce2247f798d0cccd9028cfd8 |
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| Source note | uspto-grants-2012_09 |
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