Synthon B.v.

Synthon IP Inc.

Synthon Pharmaceuticals, Inc.

Lambertus Thijs

Jie Zhu

Arjanne Overeem

Petr Benovsky

Radomir Skoumal

Jakub Castulik

Petr Bartos

Rolf Keltjens

Reinerus G Gieling

Gerrit J B Ettema

Karel Pospisilik

Gerrit Jan Bouke Ettema

Henar Tejedor Vinent

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.

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 aminoalkylphenyl carbamates, especially rivastigmine, can use less severe conditions using bis(p-nitrophenyl)carbonate (IX) as a phenol activator compound. 

Process for making aminoalkylphenyl carbamates and intermediates therefor

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

Desvenlafaxine is formed from venlafaxine by the use of a demethylating agent comprising a metal sulfide, such as sodium sulfide, and optionally selenium.

Process for making desvenlafaxine

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

Bicalutamide and/or its intermediates are made by the use of p-fluorobenzenesulfinic acid salt as a reagent.

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Wijchen, Netherlands

Lambertus Thijs