Teva Pharmaceutical Industries Limited

Anchel Schwartz

Evgeny Shapiro

Reinhard Effenberger

Asher Maymon

Judith Aronhime

Ben-Zion Dolitzky

David Leonov

Ayelet Fishman

Asher Maimon

Marko Kordova

Provided is a method of selectively enzymatically esterifying or selectively enzymatically solvolyzing epimers of analogs of vitamin D having a stereogenic center at C-24 that has a free or esterified OH group. The metod can be used, for example, for separating mixed epimers of the vitamin D analog.

Selective enzymatic esterification and solvolysis of epimeric vitamin D analog and separation of the epimers

Provided is a crystallization method for reducing the level of impurities in calcipotriene in which a solution of a starting calcipotriene in a first process solvent, for example THF, is combined with second process solvent, for example methyl formate, and, after cooling, calcipotriene is isolated. The method can include a slurry step for reducing the level of residual first process solvent.

Crystallization method for purification of calcipotriene

Provided is a method of general applicability of epimerizing a vitamin-D analog having an asymmetric allylic carbon atom at the C-24 position. The method is of particular utility in making calcipotriene.

Epimerization of analogs of vitamin D

The present invention is directed to the novel forms of torsemide, designated Form V, amorphous torsemide, Dupont Form 2 solvent adduct, Dupont Form 2 ethanol adduct and Dupont Form 2 isopropanol adduct. Methods for their preparation are also disclosed. The present invention also relates to processes for making torsemide modification I. Pharmaceutical compositions containing the new forms of torsemide and methods of using them are also disclosed.

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Rehovot, Israel

Anchel Schwartz