公开(公告)号：US08188274B2

公开(公告)日：2012-05-29

申请号：US13101195

申请日：2011-05-05

申请人： Juergen Schroeder ,  Georg Dziewas ,  Thomas Fachinger ,  Burkhard Jaeger ,  Cartsen Reichel ,  Svenja Renner

发明人： Juergen Schroeder ,  Georg Dziewas ,  Thomas Fachinger ,  Burkhard Jaeger ,  Cartsen Reichel ,  Svenja Renner

IPC分类号： C07D239/72

CPC分类号： C07D293/04

摘要： The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have 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.

摘要翻译： 本发明涉及一种制备通式（I）的氨基巴豆酰氨基取代的喹唑啉衍生物的改进方法，其中基团R a，R b，R c和R d具有权利要求中给出的含义，以及式的磺酰基衍生物及其作为 用于制备式（I）的喹唑啉的合成组分。 式（I）的喹唑啉衍生物是由酪氨酸激酶和表皮生长因子受体（EGF-R）介导的信号转导抑制剂，因此特别适用于治疗肿瘤疾病。