Rilpivirine hydrochloride
AssigneeHetero Research Foundation
InventorsBandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Adulla Venkat Narsimha Reddy, Bandi Vamsi Krishna
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Abstract
The present invention provides a novel process for the preparation of rilpivirine. The present invention also provides a novel process for the preparation of rilpivirine hydrochloride. The present invention further provides a rilpivirine hydrochloride monohydrate, process for its preparation and pharmaceutical compositions comprising it.
Claims14
A process for the preparation of rilpivirine, which comprises:
- a) condensing the (E)-3-(4-amino-3,5-dimethylphenyl)acrylonitrile hydrochloride with 4-(4-chloropyrimidin-2-ylamino)benzonitrile in the presence of N-methylpyrrolidone;
- b) heating the contents obtained in step (a) at about 75 to 95° C. to obtain a solution;
- c) cooling the solution obtained in step (b) at below 35° C.;
- d) adding water to the reaction mass;
- and
- e) isolating rilpivirine.
A process for the preparation of rilpivirine hydrochloride, which comprises:
- a. suspending rilpivirine in an alcoholic solvent;
- b. heating the contents obtained in step (a) at reflux;
- c. adding a solution of hydrochloric acid in an alcoholic solvent to the reaction mixture at reflux;
- d. maintaining the reaction mass at reflux;
- and
- e. isolating pure rilpivirine hydrochloride.
A rilpivirine hydrochloride monohydrate.
A process for the preparation of rilpivirine hydrochloride monohydrate, which comprises:
- a. suspending rilpivirine in an alcoholic solvent, a ketonic solvent or a mixture thereof;
- b. heating the contents obtained in step (a) at reflux to obtain a solution;
- c. adding carbon to the solution;
- d. removing the solvent from the solution;
- e. adding an alcoholic solvent to the residual solid obtained in step (d);
- f. passing the hydrochloride gas to the reaction mass;
- and
- g. isolating rilpivirine hydrochloride monohydrate.
A pharmaceutical composition that comprises rilpivirine hydrochloride monohydrate and pharmaceutically acceptable excipients, and optionally other therapeutic ingredients.
Dependencies are inferred from the claim text.