Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharmaceuticals, Inc.

Boehringer Ingelheim Pharma Kg

Jutta Kroeber

Joerg Brandenburg

Ralf Anderskewitz

Rogelio Perez Frutos

Rainer Soyka

Rolf Schmid

Thomas Nicola

Rainer Hamm

Yibo Xu

Rolf Bauer

Li Feng Zhang

Chris Hugh Senanayake

Jun Chi Yan

Nathan K Yee

Richard John Varsolona

Xudong Wei

Nizar Haddad

Dhileepkumar Krishnamurthy

Xiao-Jun Wang

Fabrice Gallou

Robert Simpson

Ulrich Scholz

Juergen Schnaubelt

Laurence John Nummy

Thomas Wirth

Dirk Kemmer

Dieter Gutheil

Da Deng

Robert Hagenkoetter

Michael Schul

Kai Oliver Donsbach

Diana Reeves

Juncheng Zheng

Guanghua Lv

Hans-Dieter Ecker

Eric Winter

The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I wherein Rand Rindependently denote C-alkyl groups and Xdenotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.

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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

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

The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I)wherein:

Process for preparing aryl-iminomethyl-carbamino acid esters

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Bingen, Germany

Jutta Kroeber