Process and crystalline forms of lumacaftor
AssigneeLaurus Labs Limited
InventorsRavindra Babu Bollu, Prasanta Kumar Dalasingh, Sushmita Dwarampudi, Chandrahasa Reddy Annem, Uma Maheswer Rao Vasireddi
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Abstract
The present invention generally relates to crystalline forms of Lumacaftor, processes for its preparation and pharmaceutical compositions thereof. The present invention also relates to an improved process for preparation of Lumacaftor.
Claims24
Lumacaftor Form-LA1 characterized by X-Ray diffraction (XRD) pattern having one or more peaks at about 4.3, 8.7, 12.9, 14.8, 17.5, 17.7, 18.7, 19.3, 20.3, 21.8, 22.2, 22.8, 23.5, 23.6, 25.7, 26.4, 28.0, 29.8, 33.0, 36.9, 38.2, 40.1 and 43.7±0.2° 2θ.
A process for the preparation of lumacaftor Form-LA1, comprising:
- a) dissolving lumacaftor in water and a base at a suitable temperature,
- b) optionally, cooling the solution to less than 25° C., and
- c) isolating the lumacaftor Form-LA1.
11-24. (canceled)
An improved process for the preparation of lumacaftor of Formula I,
- comprising:
- reacting a compound of Formula II with a compound of Formula III in the presence of a palladium catalyst and a base in a solvent to obtain the lumacaftor, wherein ‘X’ represent a leaving group.
33-44. (canceled)
A process for the preparation of lumacaftor Form I, comprising:
- a) suspending lumacaftor Form-LA1 in a solvent;
- and
- b) isolating the lumacaftor Form I.
Dependencies are inferred from the claim text.