PREPARATION OF CRYSTALLINE BAZEDOXIFENE AND ITS SALTS

Aspects of the present disclosure include crystalline bazedoxifene free base, crystalline bazedoxifene acetate Form D, and processes for their preparation. The drug compound having the adopted name “bazedoxifene acetate” has a chemical name 1-[4-(2-azepan-1-yl-ethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetic acid, and has the chemical structure shown below as Formula I. 124.-. (canceled)25. Crystalline bazedoxifene acetate Form D.26. The crystalline bazedoxifene acetate Form D of claim 25 , having a powder x-ray diffraction pattern with peaks located substantially in accordance with the pattern of .27. The crystalline bazedoxifene acetate Form D of having two or more powder X-ray diffraction peaks at 28 values of about 5.9 claim 25 , 7.8 claim 25 , 11.7 claim 25 , or 17.7 degrees.28. The crystalline bazedoxifene acetate Form D of having one or more additional powder X-ray diffraction peaks at 28 values of about 12.8 claim 27 , 13.4 claim 27 , 19.9 claim 27 , 23.3 claim 27 , or 34.6 degrees.29. The crystalline bazedoxifene acetate Form D of having one or more additional powder X-ray diffraction peaks at 28 values of about 9.9 claim 28 , 15.7 claim 28 , 17.1 claim 28 , or 20.5 degrees.30. A process comprising:a) providing bazedoxifene free base in an alcohol solvent, an ether solvent, an ester solvent, a ketone solvent, a halogenated hydrocarbon solvent, a hydrocarbon solvent, a nitrile solvent, a dipolar aprotic solvent, water, or any mixtures thereof;b) adding a source of acetate ions; and{'claim-ref': {'@idref': 'CLM-00025', 'claim 25'}, 'c) maintaining the mixture of step b) for a time and under conditions suitable for formation of the crystalline Form D of bazedoxifene acetate of .'}31. The process of wherein the bazedoxifene free base used in step a) is crystalline bazedoxifene free base.32. The process of wherein the source of acetate ions used in step b) is acetic acid.33. The process of claim 30 , wherein the crystallization is initiated ...

PROCESS FOR THE PREPARATION OF ROXADUSTAT AND ITS INTERMEDIATES

The present invention provides the process for the preparation of Roxadustat and its intermediates. Another aspect of the present invention provides a process for preparation of ethyl-5-(2-butoxycarbonyl)-4-phenoxyphenyl) oxazole-4-carboxylate of the formula (X) and its use in the preparation of Roxadustat. Another aspect of the present invention provides a process for the preparation of ethyl-4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate of the formula (XIII) and its use in the preparation of Roxadustat. 2) The process according to claim 1 , wherein base used in step c) is carried out in presence of a base selected from pyridine claim 1 , piperidine claim 1 , pyrimidine claim 1 , triethylamine claim 1 , tributylamine claim 1 , N-methylmorpholine claim 1 , N claim 1 ,N-diisopropylethylamine claim 1 , diethylamine claim 1 , 1 claim 1 ,1 claim 1 ,3 claim 1 ,3-tetramethylguanidine claim 1 , DBU claim 1 , DABCO.3) The process according to claim 1 , wherein acid used in step d) is carried out in presence of acid selected from hydrochloric acid claim 1 , sulphuric acid claim 1 , hydrobromic acid claim 1 , orthophosphoric acid claim 1 , Lewis acids claim 1 , AlCl claim 1 , FeCl claim 1 , acetic acid claim 1 , citric acid claim 1 , oxalic acid claim 1 , trifluoroacetic acid.5) The process according to claim 4 , wherein base used in step b) is carried out in presence of a base selected from pyridine claim 4 , piperidine claim 4 , pyrimidine claim 4 , triethylamine claim 4 , tributylamine claim 4 , N-methylmorpholine claim 4 , N claim 4 ,N-diisopropylethylamine claim 4 , diethylamine claim 4 , 2 claim 4 ,2-bipyridine claim 4 , 1 claim 4 ,1 claim 4 ,3 claim 4 ,3-tetramethylguanidine claim 4 , DBU claim 4 , DABCO.7) The process according to claim 6 , wherein the methylating reagent used in step a) is selected from trimethyl boroxine claim 6 , methylmagnesium chloride claim 6 , methyl magnesium bromide claim 6 , methyl lithium claim 6 , trimethyl silyl halides.8) The ...

Process for preparation of apremilast and its intermediates

Present application relates to the process for the preparation of 1-(3-Ethoxy-4-methoxy-phenyl)-2-methanesulf-onyl-ethylamine of the formula (II), its resolution and its use in preparation of Apremilast of formula (I), process for the preparation of crystalline form B of apremilast, process for preparation of amorphous form of apremilast and the crystalline form of (S)-1-(3-Eth-oxy-4-methoxy-phenyl)-2-methanesulfonyl-ethylamine of the formula (Va).

Preparation of bazedoxifene and its salts

Processes for preparing bazedoxifene and its pharmaceutically acceptable salts, substantially free from process related impurities and process intermediates.

Solid state forms of empagliflozin

The present invention provides solid state forms of empagliflozin, complexes of empagliflozin with amino acids, processes for their preparation and their use in purification of empagliflozin and also provided pharmaceutical compositions comprising them and their use in therapy (Formula I).

Isolated intermediate of dapagliflozin, process for the preparation of isolated intermediate of dapagliflozin, process for the preparation of dapagliflozin

Aspects of the present invention relates to an isolated intermediate of Dapagliflozin (Formula III) and its preparation, process for the preparation of Dapagliflozin, process for the preparation of crystalline propane-1,2,3-triol solvate of dapagliflozin, process for the preparation of L-proline complex of Dapagliflozin, solid premix of dapagliflozin with the polymer selected from the group consisting of eudragit, syloid, MCC Avicel PH 102 (1:1) and MCC Avicel PH 102 (1:2).

Process for preparing amorphous salts

Amorphous solid omeprazole magnesium or esomeprazole magnesium is prepared by subjecting a solution of omeprazole magnesium or esomeprazole magnesium to flash evaporation, such as by using an agitated thin film drier-vertical.

Process for the preparation of roxadustat and its intermediates

The present invention provides the process for the preparation of Roxadustat and its intermediates. Another aspect of the present invention provides a process for preparation of ethyl-5-(2-butoxycarbonyl)-4-phenoxyphenyl) oxazole-4-carboxylate of the formula (X) and its use in the preparation of Roxadustat. Another aspect of the present invention provides a process for the preparation of ethyl-4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate of the formula (XIII) and its use in the preparation of Roxadustat.

Crystalline form ii of esomeprazole magnesium trihydrate and process for its preparation

The present invention relates to crystalline form II of esomeprazole magnesium trihydrate and methods fot its preparation and use. Preferably, the crystalline form II of esomeprazole magnesium trihydrate has an X-ray powder diffraction pattern that includes five or more peaks with 2 theta angles of 4.82±0.09, 5.55±0.09, 7.41±0.09, 8.60±09, 12.10±0.09, 14.16±0.09, 18.47±0.09, and 21.08±0.09.

Process for preparation of bempedoic acid and its intermediates

The present application relates to a process for preparation of Bempedoic acid of formula (I) or its pharmaceutically acceptable salts thereof. The present application also relates to a novel intermediates of formula (II) and formula (IIA) and its application in the preparation of Bempedoic aid. The present application further relates to the crystalline form of compound of formula (IIA).

Crystalline form ii of esomeprazole magnesium trihydrate and process for its preparation

Process for the preparation of roxadustat and its intermediates

The present invention provides the process for the preparation of Roxadustat and its intermediates. Another aspect of the present invention provides a process for preparation of ethyl-5-(2-butoxycarbonyl)-4-phenoxyphenyl) oxazole-4-carboxylate of the formula (X) and its use in the preparation of Roxadustat. Another aspect of the present invention provides a process for the preparation of ethyl-4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate of the formula (XIII) and its use in the preparation of Roxadustat.