The present invention provides optical pure quinazoline compounds, especially the compounds of general formula (I), and a pharmaceutical composition containing therapeutical effective amount of the compounds. The present invention also provides the preparation of a medicament for the treatment of diseases related to the modulation of c-erbB-2 and/or EGF-R protein tyrosine kinase.本發明涉及光學純喹唑啉類化合物,特別是通式(I)的化合物,以及含有治療有效量的該化合物的醫藥組成物,及其在製備治療調節c-erbB-2及/或EGF-R蛋白酪胺酸激酶活性相關疾病的藥物中的用途。