Lek Pharmaceuticals D.d.

Other

Gorazd Sorsak

Ljubomir Antoncic

Anton Copar

A process for the preparation of amorphous atorvastatin calcium. The process includes providing a reaction mixture having a pH between 6.5 and 8.0 containing a sodium salt of atorvastatin and tetrahydrofuran. A non-cyclic chlorinated organic solvent selected from the group consisting of dichloromethane, trichloroethane, tetrachloroethane and chloroform or addition of cyclic hydrocarbon solvent selected from the group consisting of cyclohexane, cyclopentane and methyl cyclohexane is added to provide a mixture of organic solvents. An equivalent or an excess quantity of a source of calcium ions selected from the group consisting of calcium acetate and calcium chloride is added. Amorphous atorvastatin calcium is isolated from an organic phase comprising the mixture of organic solvents.

Process for the preparation of amorphous calcium salt of atorvastatin

Present invention refers to the process of preparing amorphous atorvastatin calcium without intermediate isolation of crystal or undefined mixture of crystal and amorphous atorvastatin calcium, respectively. Forming of calcium atorvastatin salt is carried out in a mixture of chlorinated organic solvent or cyclic hydrocarbon solvent, respectively, the non-hydroxylic organic solvent, and water, the source of calcium ions is calcium acetate or calcium chloride, respectively.

The invention relates to a process of preparing amorphous (4R-cis)-6-[2-[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]-dioxane-4-yl-acetic acid-tertiary butyl ester which is a useful pharmaceutical intermediate in the preparation of atorvastatin salts.

Process for preparing amorphous (4R-cis)-6-[2-[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]-dioxane-4-yl-acetic acid

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Ljubljana, Slovenia

Gorazd Sorsak