| 摘要 |
PROCESS FOR THE PREPARATION OF QUINAZOLINE DERIVATIVES The invention relates to a process for the preparation of quinazoline derivatives of the general Formula I (I) ¢wherein R1 and R2 may be the same or different and stand for hydrogen or lower alkyl or together form an ethylene (-CH2-CH2-) or trimethylene (-CH2-CH2- -CH2-) group; and n is the integer number 2 or 37 and pharmaceutically acceptable acid addition salts thereof, which comprises a) reacting an isothiourea derivative of the general Formula III (III) ¢wherein R stands for lower alkyl or phenyl-lower alkyl, where the phenyl ring of the latter group may be optionally substituted by one or more lower alkyl group(s) and/or halogen atom(s)! with an amine of the general Formula IV, (IV) (wherein R1, R2 and n are as stated above) at a temperature between 150 .degree.C and 280 .degree.C; or b) cyclising a compound of the general Formula II (II) (wherein R1, R2 and n are as stated above) optionally in the presence of a catalyst; and, if desired, converting a compound of the general Formula I thus obtained into a pharmaceutically acceptable acid addition salt thereof. |
