Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Sodium hydride | HCID 24758 | — |
| Reactant | 1-(Bromomethyl)-4-chlorobenzene | HCID 69329 | — |
| Reactant | Lithium Bromide | HCID 82050 | — |
| Reactant | HCID 178497975 | HCID 178497975 | — |
| Solvent | Water | HCID 962 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Solvent | 1,2-Dimethoxyethane | HCID 8071 | — |
| Product | HCID 58306504 | HCID 58306504 | — |
| Product | HCID 58306546 | HCID 58306546 | — |
Reaction Steps
To a mixture of ice-cooled methyl 6-hydroxypyridine-2-carboxylate (800 mg), DME (10.5 mL), and DMF (2.6 mL) was added sodium hydride (55% oil dispersion, 240 mg), followed by stirring for 10 minutes. To this was added lithium bromide (910 mg), and then the mixture was stirred at room temperature for 15 minutes and further 4-chlorobenzylbromide (2.15 g) was added thereto. This mixture was stirred at 65° C. for 20 hours. Water was added thereto, followed by extraction with ethyl acetate-diethyl ether, and the organic layer was washed with water and saturated brine in this order, and dried over anhydrous sodium sulfate. The solvent was evaporated, and the obtained residue was purified by silica gel column chromatography (hexane-ethyl acetate) to obtain methyl 1-(4-chlorobenzyl)-6-oxo-1,6-dihydropyridine-2-carboxylate (270 mg; Example 41a) and methyl 6-[(4-chlorobenzyl)oxy]pyridine-2-carboxylate (448 mg; Example 41b), as a colorless oily substance, respectively.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US08598355B2 |
|---|
| Source dataset | uspto-grants-2013_12 |
|---|
| ORD ID | ord-a477b5d8112440a091cdac3a7e1436d9 |
|---|
| Source note | uspto-grants-2013_12 |
|---|