Teva Pharmaceutical Industries Limited

Neomi Gershon

Judith Aronhime

Claude Singer

Tamar Nidam

Marioara Mendelovici

Ben-Zion Dolitzky

Valerie Niddam-Hildesheim

Nissim Garti

Eduard Schwartz

Gideon Pilarsky

Ilya Avrutov

Yana Berkovich

Anita Liebermann

Shlomit Wizel

Anita Liberman

Gideon Pilarski

Ehud Amir

Arina Ceausu

Anita Lieberman

Iiya Avrutov

Greta Sterinbaum

Marioura Mendelovici

The invention provides a method for preparing levofloxacin hemihydrate, comprising: The invention also provides a method of converting a levofloxacin form to levofloxacin hemihydrate, comprising storing one or more forms selected from the group consisting of Forms A, B, C, F, G and H for a sufficient time to permit the one or more forms to convert to levofloxacin hemihydrate.

Preparation of levofloxacin and hemihydrate thereof

The invention provides a process for preparing levofloxacin hemihydrate, comprising:

Methods for the purification of levofloxacin

The present invention relates to lamotrigine, a useful agent for anti-epilepsia. New crystal forms of lamotrigine containing molecules of the solvent in stoichiometric ratios are disclosed. The present invention also provides processes for preparing the new crystal forms of lamotrigine.

Crystal forms of lamotrigine and processes for their preparations

The present invention relates to a process of preparing benzisoxazole methane sulfonic acid-chloride (BOS&#x2014;Cl) as an zonisamide intermediate via chlorination of benzisoxazole methane sulfonate. The present invention also discloses a process of preparing zonisamide via amidation of BOS&#x2014;Cl. More particularly, the present invention provides a process of preparing zonisamide, comprising the steps of: a) chlorinating BOS, salts or esters thereof, with SOClin an organic solvent and/or in the presence of a catalyst to form BOS&#x2014;Cl; and b) amidating BOS&#x2014;Cl in the presence of ammonia selected from the group consisting of aqueous ammonia in a biphasic system, masked ammonia and dry ammonia to form zonisamide.

Method for preparing benzisoxazole methane sulfonyl chloride and its amidation to form zonisamide

The present invention provides an improved process for preparing modafinil, whereby it may be isolated in high purity by a single crystallization. The process produces modafinil free of sulphone products of over-oxidation and other byproducts. The invention further provides new crystalline Forms II-VI of modafinil and processes for preparing them. Each of the new forms is differentiated by a unique powder X-ray diffraction pattern. The invention further provides pharmaceutical compositions containing novel modafinil Forms II-IV and VI.

Oxidation method for preparing highly pure modafinil, crystalline forms of modafinil, and methods of preparing the crystalline forms

The present invention is directed to (&plus;)-cis-sertraline hydrochloride and methods of preparation. The present invention also includes processes for making sertraline having a cis/trans ratio greater than 3:1, greater than or equal to 8:1, or between about 8:1 and about 12:1, from the Schiff base of sertralone, sertraline-1-imine.

Process for preparing (&plus;)-cis-sertraline

New leflunomide Form III is disclosed, along with processes for preparing it. The present invention also provides an economic process for preparing leflunomide Form II and a process for preparing leflunomide Form I from leflunomide Form III. Pharmaceutical compositions and dosage forms containing the new form and methods of using them for the treatment of rheumatoid arthritis are also disclosed.

Process for preparing leflunomide form I

A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided in which the carboxylic acid group of 5-methylisoxazole-4-carboxylic acid is chlorinated, forming 5-methylisoxazole-4-carboxylic acid chloride. The acid chloride is then reacted without intermediate distillation with 4-trifluoromethylaniline in the presence of an alkali metal or alkaline-earth metal bicarbonate acid scavenger.

Method for synthesizing leflunomide

Processes for making- and a new crystalline form of- leflunomide

A process for the preparation of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate, and the product produced thereby, comprising reacting by heating 2-chloro-4-amino-6,7-dimethoxyquinazoline and 1-(2-tetrahydrofuroyl)piperazine in a polar organic reaction solution, wherein the polar organic reaction solution comprises a polar organic solvent and a minimum amount of water effective to produce 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate. The heat is added, preferably at reflux for a period of time, after which the reaction solution is allowed to cool to room temperature and the crystalline product 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate is filtered and dried.

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Kfar Saba, Israel

Neomi Gershon