Synthon B.v.

Synthon IP Inc.

Synthon Pharmaceuticals, Inc.

Jie Zhu

Lambertus Thijs

Arjanne Overeem

Petr Benovsky

Radomir Skoumal

Jakub Castulik

Petr Bartos

Reinerus G Gieling

Frantisek Picha

Rolf Keltjens

Judith Firet

Judith Janneke Firet

Thijs Lambertus

The compound of formula (8), in racemic or single enantiomeric form, is useful in making N-(diphenylmethyl)-piperazines such as cetirizine and levocetrizine. 

Process for making n-(diphenylmethyl)piperazines

Asenapine and related trans-isomer bicyclic compounds can be obtained by reducing a compound of formula (C) to preferentially form a trans-isomer compound of formula (D), followed by subsequent ring closure to form a compound of formula (B) such as asenapine. 

Process for making asenapine

A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (20) is provided.

Process for making montelukast and intermediates therefor

A compound of the following formula wherein R' is a straight or branched C1-C4 alkyl group is useful in processes associated with the synthesis of montelukast and its salts.

The reaction of methylmagnesium halide is improved by the presence of a cerium (III) salt such as cerium trichloride. The reactions are typically associated with the production of montelukast, a pharmaceutically useful compound of the following formula and salts thereof. Further enhancements can be derived from certain intermediates, salts thereof and/or purification thereof before and/or after the reaction involving methylmagnesium halide.

The (S)-citalopram content of a mixture of (R)- and (S)-citalopram can be enriched by using L-tartaric acid as the resolving agent in the presence of formaldehyde.

Process for resolving citalopram

Pioglitazone can be made via a Darzens Condensation reaction in an industrially useful process.

Processes for making pioglitazone and compounds of the processes

A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (4) is provided.

A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (11) is provided.

Water-soluble salts of pioglitazone especially pioglitazone sulfate are useful in pharmaceutical applications.

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Nijmegen, Netherlands

Jie Zhu