HuagongsheHuagongshe Chemistry Print Report · For research reference only
3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methylpyrido[1,2-a]pyrimidin-4-one → Paliperidone
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methylpyrido[1,2-a]pyrimidin-4-one | HCID 44602517 | — |
| Catalyst | Palladium | HCID 23938 | — |
| Catalyst | Platinum | HCID 23939 | — |
| Solvent | Acetic Acid | HCID 176 | — |
| Product | Paliperidone | HCID 115237 | — |
Reaction Steps
In the step-b, the pyridine ring of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-4H-pyrido-[1,2-a]pyrimidin-4-one, compound of formula-11, is reduced by a suitable reducing agent as defined earlier. Good yields were obtained on hydrogenation using palladium or platinum catalyst in acidic conditions. In the preferred embodiment the reaction was performed by hydrogenation using palladium catalyst in presence of acetic acid to provide pure paliperidone.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08481729B2 |
| Source dataset | uspto-grants-2013_07 |
| ORD ID | ord-d4b4278f66ed4b56859946c4f2d53a6d |
| Source note | uspto-grants-2013_07 |