Process for preparation of tafamidis and salts thereof
AssigneeAlivus Life Sciences Limited
InventorsVenkata Raghavendra Charyulu Palle, Suresh Mahadev Kadam, Vishweshwar Peddy, Santosh Ramesh Badgujar, Vinayak Kacheshwar Bhujade, Yogesh Eknath Gagare
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Abstract
The present invention relates to process for preparation of crystalline Form 4 of tafamidis. The present invention also relates to salts of tafamidis and process of preparation of salts of tafamidis. The present invention also relates to process for preparation of an amorphous solid dispersion of tafamidis or salt thereof.
Claims13
A process for the preparation of crystalline Form 4 of tafamidis, the process comprising:
- (a) providing a solution of tafamidis in a solvent selected from the group consisting of C1-C4 amides, C2-C3 sulfoxides, C5-C6 pyrrolidones, and mixtures thereof;
- and
- (b) obtaining a crystalline Form 4 of tafamidis from the solution of step (a) by:
- (i) combining the solution of step (a) with an anti-solvent selected from the group consisting of C1-C8 alcohols, C3-C10 ketones, C1-C3 nitriles, water and mixtures thereof;
- or
- (ii) removing the solvent from the solution of step (a),
- wherein the crystalline Form 4 of tafamidis is characterized by an X-ray powder diffraction (XRPD) pattern as illustrated in FIG. 1.
A process for the preparation of a salt of tafamidis, the process comprising:
- (a) reacting tafamidis with an inorganic base or an organic base to form a reaction mixture comprising the tafamidis salt;
- and
- (b) separating the tafamidis salt from the reaction mixture of the step (a),
- wherein the tafamidis of step (a) is obtained by reacting 4-(3,5-dichlorobenzamido)-3-hydroxybenzoic acid with methanesulfonic acid in an amide solvent.
Dependencies are inferred from the claim text.