| 摘要 |
<p>Quinazoline derivs. of formulae (I) and (II) and their acid addn. salts X,Y = H, OH, halogen, CF3, 1-4C alkyl/alkoxy; or X+Y=benzo, CH2O2, C2H4O2. R1,2 = H, 1-6C alkyl, aryl/aralkyl opt. substd. hydrocarbyl, 2-4C alkenyl, (1-3C alkyl)2N-(2-4C)alkyl; or R1+2 = 3-7C cycloalkyl. R3 = H, 1-4C alkyl, aryl/aralkyl hydrocarbyl opt. substd. R4 = morpholine, 1-6C alkylpiperazine, 2-4C alkenylpiperazine, phenylpiperazine opt. substd. on Ph by halogen, CF3, 1-6C alkyl/alkoxy. (a) A mixt. of 2-diethylamino-6,7-dimethoxy-4(3H)-quinazolone.HCl (10 g) and POCl3 (50ml) is refluxed for 2 hrs. to give the 4-chloro cpd.(7.6 g). (b) the HCl salt of this (34.1 g.) in EtOH (500 ml) with 10% Pd-C (1.5 g.) is hydrogenated to give 2-diethylamino-3,4-dihydro-6,7-dimethoxyquinazoline. HCl (77%), crystd. from EtOAc-MeOH.</p> |
