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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 448535Generated: October 29, 2026

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

https://huagongshe.com/reaction/448535

Reaction equation

Participants

RoleNameHCIDCharge
Reactant3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methylpyrido[1,2-a]pyrimidin-4-oneHCID 44602517—
CatalystPalladiumHCID 23938—
CatalystPlatinumHCID 23939—
SolventAcetic AcidHCID 176—
ProductPaliperidoneHCID 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

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08481729B2
Source datasetuspto-grants-2013_07
ORD IDord-d4b4278f66ed4b56859946c4f2d53a6d
Source noteuspto-grants-2013_07