HuagongsheHuagongshe Chemistry Print Report · For research reference only
4,6-Dichloro-5-methylpyrimidine → 5-(4-(6-Chloro-5-methylpyrimidin-4-yloxy)piperidin-1-yl)-3-isopropyl-1,2,4-oxadiazole
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4,6-Dichloro-5-methylpyrimidine | HCID 818860 | — |
| Reactant | 1-(3-Isopropyl-1,2,4-oxadiazol-5-YL)piperidin-4-OL | HCID 21897744 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Solvent | Potassium tert-butoxide | HCID 23665647 | — |
| Product | 5-(4-(6-Chloro-5-methylpyrimidin-4-yloxy)piperidin-1-yl)-3-isopropyl-1,2,4-oxadiazole | HCID 86597366 | 72.3% |
Reaction Steps
To a solution of 1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-piperidin-4-ol (3.65 g, 17 mmol) and 4,6-dichloro-5-methylpyrimidine (2.83 g, 17 mmol) in THF (70 mL), 1M potassium-t-butoxide in THF (16 mL, 16 mmol) was added dropwise. The mixture was stirred at room temperature for 10 min. The crude mixture was purified by column chromatography on silica gel with hexane/ethyl acetate (3:1 v/v) to provide 4-chloro-6-[1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-piperidin-4-yloxy]-5-methyl-pyrimidine as a solid (4.15 g, 71%). Exact mass calculated for C15H20ClN5O2337.13, found 338.2 (MH+).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08546429B2 |
| Source dataset | uspto-grants-2013_10 |
| ORD ID | ord-1f34800992164151a3f8684e44b0c7bf |
| Source note | uspto-grants-2013_10 |