摘要 |
Quinazolinediamines I(R1,R2=alkyl, alkenyl, alkynyl, hydroxyalkyl; NR1R2=heterocyclic; Y1 =H, Cl, Y2=alkoxy; Y3=H, alkoxy) were prepd. Thus, 5-chloro-4-methoxyanthranilic acid was treated with KOCN to give 6-chloro-7-methoxy-2, 4-quinazolinedione, which was chlorinated with PCl5-POCl3, then treated with NH3 and 2-methyl-2-hydroxypropyl piperazine carboxylate to give I≮NR1R2 = 4-(2-hydroxy-2-methylpropoxy carbonyl) piperazino; Y1=Cl; Y2=OMe; Y3=H≉(II). At 0.2 mg/kg orally in dogs II gave a decrease in blood pressure of 40 mmHg. |