Synthon B.v.

Jakub Castulik

Jie Zhu

Lambertus Thijs

Arjanne Overeem

Petr Benovsky

Radomir Skoumal

Petr Bartos

Libor Vyklicky

Miroslav Zabadal

Zdenek Jelinek

The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group. 

Process for making bortezomib and intermediates for the process

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

Jakub Castulik