Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Oxalic Acid | HCID 971 | — |
| Reactant | 3-Hydroxypyridine | HCID 7971 | — |
| Reactant | Tetrahydrofuran | HCID 8028 | — |
| Reactant | 1-Piperidinecarbonyl chloride | HCID 242085 | — |
| Catalyst | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| Solvent | Ethanol | HCID 702 | — |
| Solvent | Water | HCID 962 | — |
| Product | HCID 69378687 | HCID 69378687 | 61.2% |
Reaction Steps
3-Hydroxypyridine (400 mg), TEA (1.17 ml) and DMAP (catalytic amount) were added in that order to a THF (10 ml) solution containing piperidine-1-carbonyl chloride (745 mg), and then heated at 60° C. for 5 hours. The reaction solution was cooled, then water (3 ml) was added thereto, and extracted with EtOAc. The extract was washed with water, and then dried over anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel column chromatography (eluent: hexane:EtOAc=1:1 (v/v)) to obtain a colorless oil. The resulting oil was dissolved in ethanol, and an ethanol solution of oxalic acid (378 mg) added thereto to obtain a colorless powder. This was recrystallized from hexane/ethanol to obtain (pyridin-3-yl)piperidine-1-carboxylate oxalate (761 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07919494B2 |
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| Source dataset | uspto-grants-2011_04 |
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| ORD ID | ord-c85b2491525047b6bfd4c9ef77666c95 |
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| Source note | uspto-grants-2011_04 |
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