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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2280430Generated: October 28, 2026

Methane → Rilpivirine hydrochloride

https://huagongshe.com/reaction/2280430

Reaction equation

Participants

RoleNameHCIDCharge
ReactantMethaneHCID 297—
ReactantHydrochloric AcidHCID 313—
ReactantRilpivirineHCID 6451164—
SolventMethanolHCID 887—
SolventIsopropanolHCID 3776—
SolventMethyl Ethyl KetoneHCID 6569—
ProductRilpivirine hydrochlorideHCID 11711114—

Reaction Conditions

Temperature62.5 °C

Reaction Steps

Rilpivirine (20 gm; Chromatographic purity: 96.5%) was suspended in a mixture of methanol and methyl ethyl ketone (1:1, 2000 ml) and then heated to reflux for 1 hour to provide a clear solution. The solution was treated with charcoal and filtered through celite bed. The solvent was distilled off under reduced pressure to obtain a residual solid. To the residual solid was added methanol (200 ml) and then heated to 60 to 65° C. To the solution was added a solution of hydrochloric acid in isopropanol (200 ml) at 60 to 65° C. and stirred for 1 hour 30 minutes. The contents were cooled to room temperature and stirred for 30 minutes. The separated solid was filtered and then dried to provide 14 gm of rilpivirine hydrochloride.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09139535B2
Source datasetuspto-grants-2015_09
ORD IDord-83b3be3bfaaa40a09965ecec7c8f2a08
Source noteuspto-grants-2015_09