Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharmaceuticals, Inc.

Boehringer Ingelheim Pharma Gmbh & Co Kg

Thomas Nicola

Dirk Kemmer

Peter Sieger

Martin Renz

Peter Kohlbauer

Waldemar F Pfrengle

Adil Duran

Thorsten Pachur

Rogelio Perez Frutos

Thomas Wirth

Yibo Xu

Jutta Kroeber

Li Feng Zhang

Chris Hugh Senanayake

Nathan K Yee

Richard John Varsolona

Xudong Wei

Nizar Haddad

Dhileepkumar Krishnamurthy

Xiao-Jun Wang

Fabrice Gallou

Robert Simpson

Juergen Schnaubelt

Laurence John Nummy

Joerg Brandenburg

Michael Brenner

Dieter Gutheil

Diana Reeves

Michael Schul

Robert Hagenkoetter

Michael Wiese

Kai Donsbach

Kai Oliver Donsbach

Eric Winter

Thomas Herweck

Albrecht Jacobi

Hans-Dieter Ecker

The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

Polymorphs

The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.

Process for the preparation of chiral 8-(3-aminopiperidin-1-yl)-xanthines

The invention relates to a process for carrying out metathesis reactions, wherein the process is carried out continuously and a ruthenium-containing catalyst is used.

Process for continuous ruthenium-catalysed metathesis

The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. The process involves reacting a compound of the formula (III) with 3-(phthalimido)piperidine or an enantiomer thereof where X is a leaving group selected from halogens and sulphonic ester acid residues, and Rto Rare as defined herein, to obtain a compound of the formula (II) and deprotecting the obtained compound of the formula (II) to obtain the product xanthines.

Process for the preparation of chiral 8-(-3-aminopiperidin-1-yl) xanthines

Disclosed is a multi-step process for preparing a compound of Formula I: wherein Rto Rare as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.

Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides

A process of diminishing the concentration of a transition metal complex from a first solution by adding a solubility-enhancing compound that enhances the solubility of said complex in a second solution and extracting the first solution with the second solution. The solubility-enhancing compound is a compound of formula A wherein,

Process of removing transition metals

Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, Rthrough R, D, A and Rare as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

Process for preparing macrocyclic compounds

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Mainz, Germany

Thomas Nicola