Savelli F, Pirisino G, Alamanni M C, Manca P, Satta M
Farmaco Sci. 1983 Nov;38(11):869-76. doi: 10.1002/chin.198342245.
By condensating ethyl pyruvate with 4-dialkylaminoalkyl-5-aminopyrimidine, obtained by hydrogenolysis of the corresponding 6-chloroderivatives, were prepared 3-methyl-6,8-diazaquinoxalinee-2(1H)-ones which carry on position 1 a tert-aminoalkyl chain (dimethylaminoethyl-, morpholinylethyl-, dimethylaminopropyl- and N-methylpiperazinylpropyl-). The synthetized compounds were tested to verify the effects on acquisition and modification of a conditioned avoidance response (C.A.R.) in rats. In these tests 1-dimethylaminoethyl-3-methyl-6,8-diazaquinoxalin-2(1H)-one, shows activity comparable with that of the cloropromazine.
通过将丙酮酸乙酯与由相应的6-氯衍生物氢解得到的4-二烷基氨基烷基-5-氨基嘧啶缩合，制备了在1位带有叔氨基烷基链（二甲基氨基乙基、吗啉基乙基、二甲基氨基丙基和N-甲基哌嗪基丙基）的3-甲基-6,8-二氮杂喹喔啉-2(1H)-酮。对合成的化合物进行了测试，以验证其对大鼠条件性回避反应（C.A.R.）的习得和改变的影响。在这些测试中，1-二甲基氨基乙基-3-甲基-6,8-二氮杂喹喔啉-2(1H)-酮显示出与氯丙嗪相当的活性。
