Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Thomas Fachinger

Svenja Renner

Carsten Reichel

Burkhard Jaeger

Juergen Schroeder

Georg Dziewas

Rolf Schmid

Juergen Schnaubelt

Thomas Krueger

Joern Merten

Michael Konrad

Emanuel Stehle

Bianca Werner

Cartsen Reichel

A process for preparing compounds of the formula (I) in which Rand Rare as defined in the description.

Preparation process

The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups R, R, Rand Rhave the meanings given in the claims, as well as sulphonyl derivatives of formula and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.

Process for preparing aminocrotonylamino-substituted quinazoline derivatives

The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups R, R, Rand Rhave the meanings given in the claims, as well as sulphonyl derivatives of formula (XIII) and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases. 

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Niederheimbach, Germany

Thomas Fachinger