HuagongsheHuagongshe Chemistry Print Report · For research reference only
Sodium Carbonate → 2-tert-Butoxy-3-[2-[4-(2-fluorophenoxymethyl)piperidino)ethyl]pyrazine
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Sodium Carbonate | HCID 10340 | — |
| Reactant | Sodium triacetoxyborohydride | HCID 5049666 | — |
| Reactant | 4-((2-Fluorophenoxy)methyl)piperidine hydrochloride | HCID 17178050 | — |
| Reactant | (Z)-2-tert-butoxy-3-(2-methoxyvinyl)pyrazine | HCID 67047587 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Solvent | Ethyl Acetate | HCID 8857 | — |
| Product | 2-tert-Butoxy-3-[2-[4-(2-fluorophenoxymethyl)piperidino)ethyl]pyrazine | HCID 22247861 | 10.1% |
Reaction Steps
After adding 139 mg of (Z)-2-tert-butoxy-3-(2-methoxyvinyl)pyrazine and 196 mg of 4-(2-fluorophenoxymethyl)piperidine hydrochloride in 5 ml of dichloromethane, 213 mg of sodium triacetoxyborohydride was added and the mixture was stirred overnight at room temperature. Aqueous sodium carbonate solution was added to the reaction mixture and extraction was performed with ethyl acetate. The organic layer was washed with water and saturated brine in that order and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane/ethyl acetate) to obtain the title compound (26 mg, 10% yield).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07265108B2 |
| Source dataset | uspto-grants-2007_09 |
| ORD ID | ord-70668521291d428a9e88092522c8e7e7 |
| Source note | uspto-grants-2007_09 |