Synthon B.v.

Radomir Skoumal

Lambertus Thijs

Jie Zhu

Arjanne Overeem

Petr Benovsky

Jakub Castulik

Petr Bartos

Petr Melsa

The present invention relates to a process for preparation of crystalline Form 1 of gefitinib of formula (1) characterized by a XRPD powder diffraction pattern comprising, inter alia, peaks at about 7.14, 11.26, 14.25, 15.86, 24.33 and 26.40 degrees 2 theta (&#xb1;0.2 degrees 2 theta), the process comprising the steps: 1. Dissolving gefitinib in a solvent mixture comprising water and an alcohol selected form ethanol and butanol, wherein the ratio between water and alcohol is between 1:16 and 1:25 (vol:vol) 2. Isolating gefitinib Form 1. 

Process for making crystalline form a of gefitinib

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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Blansko, Czechia

Radomir Skoumal