Toja E, Omodei-Salé A, Corsico N
Farmaco Sci. 1984 May;39(5):450-62.
The synthesis and activity on the central nervous system of a series of 2-aryl or 2-alkyl-7-phenylhexahydroimidazo[1,5-a] pyrazin-3(2H)-ones (II a-f) are reported. The intermediate 3-carbomethoxy-1-phenylpiperazine (X) was prepared in six steps from aniline and methyl-2-chloroacrylate. Compared with that of derivatives of Zetidoline, the depressant activity of (II a-f) is markedly reduced.
报道了一系列2-芳基或2-烷基-7-苯基六氢咪唑并[1,5-a]吡嗪-3(2H)-酮(II a-f)的合成及其对中枢神经系统的活性。中间体3-甲氧羰基-1-苯基哌嗪(X)由苯胺和甲基-2-氯丙烯酸酯经六步反应制得。与泽替多林的衍生物相比,(II a-f)的抑制活性明显降低。