Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Goesta Rimmler

Ursula Hoffmann

Hans Hilpert

Mark Rogers-Evans

Peter John Harrington

Pius Waldmeier

Fabienne Hoffmann-Emery

Pirmin Hidber

David A Johnston

Lewis M Hodges

Helmut Werner Stahr

Franziska E Rohrer

Michael Hennig

Andre Bubendorf

Wolfgang Goehring

Andre Gerard Bubendorf

André Gerard Bubendorf

A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.

Process for the production of acid chlorides

The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described hereinwhich comprises the steps of with a compound of formula to form a compound of formula b) converting the OH/&#x2550;O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl, PBr, MeI and (FCSO)O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; and The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.

Process for preparation of pyridine derivatives

The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.

[6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride polymorph

A process is described for preparing certain 4-alkyl- or 4-aryl-pyridine derivatives.

Process for the preparation of pyridine derivatives

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Bad Krozingen, Germany

Goesta Rimmler