Rigel Pharmaceuticals, Incorporated

Dsm IP Assets B.v.

Newron Pharmaceuticals S.p.a.

Dsm Sinochem Pharmaceuticals Netherlands B.v.

Dpx Holdings B.v.

Michael Wolberg

Karl-Heinz Giselbrecht

Daniel Mink

Ulfried Felfer

Peter Hans Riebel

Wolfgang Skranc

Ben De Lange

Dennis Heemskerk

Erwin Waldvogel

Wilhelmus Hubertus Joseph Boesten

Natascha Sereinig

Christoph Imboden

Peter Hans Ermann

Andreas Hendrikus Maria De Vries

Petrus Johannes Hermsen

Ulfried Feifer

Matthias Riepl

The present invention relates to a new process for the production of substituted 2-[2-(phenyl) ethylaminojalkaneamide derivatives of the following formula (I), in particular 2-[2-(3-butoxyphenyl)-ethylamino]-N,N-dimethylacetamide in high yields with very high chemical purity. The invention relates to a process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof:

Process for the production of substituted 2-[2-(phenyl) ethylaminojalkaneamide derivatives

The present invention relates to a process for the preparation of a diol sulfone derivative comprising reaction of a halomethyl substrate with a thio-aryl compound to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.

Process for the preparation of diol sulfones

This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The invention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.

Synthesis of R-biphenylalaninol

Disclosed herein are methods for synthesizing 2,4-pyrimidinediamines as well as intermediates used therein.

Synthesis of 2,4-pyrimidinediamines

The invention relates to a process for the preparation of (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile from 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one, wherein X stands for a leaving group, by reacting 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one with a cyanide ion in water and by subsequent lowering of the pH to a pH between 0 and 5. (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable from (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile may suitably be used in the preparation of a pharmaceutical preparation, more in particular in the preparation of statins, more in particular in the preparation of Atorvastatine or a salt thereof, for instance its calcium salt. The invention also relates to (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable therefrom.

Process for the preparation of (4-hydroxy-6-oxo-tetrahydropyran-2-yl) acetonitrile and derivatives

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Neutraubling, Germany

Michael Wolberg