目的 設(shè)計(jì)并合成吡唑并嘧啶類(lèi)化合物，并對(duì)其進(jìn)行催眠作用研究。方法 以乙酮類(lèi)衍生物和N，N-二甲基甲酰胺二甲基縮醛為起始原料，再與3-氨基-4-氰基吡唑反應(yīng)制備一系列吡唑并嘧啶類(lèi)化合物；分別對(duì)閾下劑量戊巴比妥鈉所致小鼠的催眠作用和閾上劑量戊巴比妥鈉所致小鼠的催眠作用進(jìn)行研究。結(jié)果 設(shè)計(jì)并合成了7個(gè)目標(biāo)化合物，其結(jié)構(gòu)經(jīng)¹H-NMR和ESI-MS確證。閾下劑量戊巴比妥鈉所致小鼠的催眠作用研究表明化合物AL-5、AL-7有一定的協(xié)同戊巴比妥鈉的催眠作用（P<0.05），化合物AL-1、AL-3具有明顯的催眠作用（P<0.01）。閾上劑量戊巴比妥鈉所致小鼠的催眠作用研究表明AL-1、AL-3、AL-5和AL-7組的睡眠持續(xù)時(shí)間均顯著延長(zhǎng)（P<0.01、0.05），表明這些化合物有鎮(zhèn)靜催眠的效果。結(jié)論 改進(jìn)了吡唑并嘧啶類(lèi)化合物的合成工藝，操作簡(jiǎn)單、成本低、產(chǎn)率較高；通過(guò)小鼠的行為學(xué)觀(guān)察法對(duì)化合物的藥效做了初步的評(píng)價(jià)，為今后的合成研究提供了方向。

Objective To design and synthesize pyrazolopyrimidine derivatives, and to study their hypnotic activities. Methods Ethyl ketone derivatives and N, N-dimethylformamide dimethyl acetal were used as the starting material, and reacted with 3-aminopyrazole-4-carbonitrile to synthesize the target compounds. The hypnotic activities of subliminal dose and threshold dose of pentobarbital sodium in mice were studied. Results Seven targeted compounds were designed and synthesized, and their chemical structures were confirmed by ¹H-NMR and ESI-MS. The study on hypnotic activities of subliminal dose of pentobarbital sodium in mice showed that compounds AL-5 and AL-7 had cooperated with the hypnotic effect of pentobarbital sodium (P < 0.05). And compounds AL-1 and AL-3 had the significant hypnotic activities (P < 0.01). The study on hypnotic activities of threshold dose of pentobarbital sodium in mice showed that sleep duration in AL-1, AL-3, AL-5, and AL-7 groups were significantly prolonged (P < 0.05, 0.01), indicating these compounds had the hypnotic activities. Conclusion This study improves the synthesis process of pyrazolopyrimidine derivatives with simple operation, low cost, and high yield. And the pharmacodynamics of these compounds are preliminary evaluated through the behavioral observation method of mice, and to provide the direction for future synthesis research.