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US 2025/0129039 A1Published application
Novel process for the preparation of bilastine and intermediates thereof
AssigneeBiophore India Pharmaceuticals PVT. Ltd.
InventorsManik Reddy PULLAGURLA, Bhaskar Reddy PITTA, Jagadeesh Babu RANGISETTY
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Abstract
A novel process for the preparation of 2-[4-[2-[4-[1-(2-ethoxyethyl) benzimidazol-2-yl] piperidin-1-yl] ethyl]phenyl]-2-methyl propionic acid (I) is provided. A process for the purification of Bilastine (I), having purity greater than 99.0% by High performance liquid chromatography (HPLC) is also provided.
Claims11
A process for the preparation of Bilastine (I), comprising:
- i. acetylation of 2-phenylethanol (V) in presence of suitable acetylating reagent and aluminium chloride to form compound (VI);
- wherein, R is defined as COCH(CH3)2 or COCH3,
- ii. conversion of compound (VI) in presence of a suitable oxidative reagent and a metal halide to form compound (VII);
- wherein, R is defined as COCH(CH3)2 or COCH3;
- R1 is C1-C4 alkyl.
- iii. hydrolysis of compound (VII) in the presence of a suitable base to form compound (VIII);
- wherein, R is defined as COCH(CH3)2 or COCH3;
- R1 is C1-C4 alkyl.
- iv. conversion of compound (VIII) with a suitable reagent to form compound (II);
- wherein, R1 is C1-C4 alkyl;
- R2 is halo or SO3CH3
- v. coupling of compounds (II) with 1-(2-ethoxyethyl)-2-(piperidin-4-yl)-1H-benzo[d]imidazole (III) in presence of a suitable base to form compound (IV);
- wherein, R1 is C1-C4 alkyl;
- R2 is halo or SO3CH3
- and
- vi. hydrolysis of compound (IV) with a suitable base to obtain Bilastine (I), wherein the Bilastine (1) obtained has total impurities less than 0.5% (w/w).
13 more elements
A process for the purification of Bilastine (I), comprising:
- a) providing Bilastine (I), in a suitable solvent.
- b) heating the reaction mixture to a suitable temperature.
- c) cooling the reaction mass;
- and
- d) isolating pure Bilastine (I).
2 more elements
A compound of formula (VII)
- where R is defined as COCH(CH3)2, or COCH3, R1 is C1-C4 alkyl.
Dependencies are inferred from the claim text.