Synthon B.v.

Synthon IP Inc.

Synthon Pharmaceuticals, Inc.

Arjanne Overeem

Lambertus Thijs

Jie Zhu

Petr Benovsky

Radomir Skoumal

Jakub Castulik

Petr Bartos

Reinerus G Gieling

Dennie J M Van Den Heuvel

Henar Tejedor Vinent

Thijs Lambertus

The invention deals with a novel process for making the pharmaceutically useful product Sugammadex of formula (1) 

Process for making Sugammadex

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.

A solid form of a compound of formula 1: is provided. The compound of formula 1 can be obtained in solid state by precipitation from a solution containing the same. The compound is useful as leukotriene antagonist and can be formulated into a pharmaceutical composition that also includes a pharmaceutically acceptable excipient.

Solid-state montelukast

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.

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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Ede, Netherlands

Arjanne Overeem