Synthon B.v.

Petr Bartos

Lambertus Thijs

Jie Zhu

Jiri Bartl

Arjanne Overeem

Petr Benovsky

Radomir Skoumal

Jakub Castulik

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.

Process for making montelukast and intermediates therefor

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.

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

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Brno, Czechia

Petr Bartos