1-[二-(4-氟苯)甲基]哌嗪衍生物的合成.docVIP

1-[二-（4-氟苯）甲基]哌嗪衍生物的合成 [关键词]哌嗪类/化学合成；1-[二-（4-氟苯）甲基]哌嗪衍生物； [摘要]目的：1-[二-（4-氟苯）甲基]哌嗪衍生物的合成。方法：以哌嗪为起始原料，通过与[二-（4-氟苯)]甲基氯反应得到1-[二-（4-氟苯）甲基]哌嗪Ⅰ，Ⅰ分别经过与氯乙酸乙酯和4-氯乙酰乙酸乙酯反应得到2-[二-（4-氟苯）甲基]哌嗪乙酸乙酯Ⅱ和2-[二-（4-氟苯）甲基]哌嗪乙酰乙酸乙酯Ⅲ。Ⅲ再与醛和硫脲在催化剂的催化下反应得到最终产物Ⅳ。结果：改进了关键的中间体Ⅰ的合成方法，使它的收率由文献的54%提高到90.1%。并制备合成了5种1-[二-（4-氟苯）甲基]哌嗪衍生物。结论：1-[二-（4-氟苯）甲基]哌嗪衍生物值得更进一步的深入研究。 1 - [2 - (4 - fluorine benzene) methyl] piperazines derivatives synthesis KEY WORDS Piperazines/chem syn;1 - [2 - (4 - fluorine benzene) methyl] piperazine derivatives SUMMARY OBJECTIVE:Purpose: 1 - [2 - (4 - fluorine benzene) methyl] piperazine derivatives synthesis .Methods:With piperazine as the starting material, with [2 - (4 - fluorine benzene)] methyl chloride hydrochloride.results 1 - [2 - (4 - fluorine benzene) methyl] piperazine Ⅰ, Ⅰ respectively after 4 - chloride and ethyl chloroacetate and ethyl acetoacetate react to get 2 - [2 - (4 - fluorine benzene) methyl] piperazine ethyl acetate Ⅱ and 2 - [2 - (4 - fluorine benzene) methyl] piperazine ethyl acetoacetate Ⅲ. Ⅲ again with aldehyde and thiourea in catalyst Ⅳ catalytic reaction to obtain the final product.Results:Improved the synthetic methods of the key intermediates Ⅰ, make its yield rose to 90.1% from 54% the literature. And the preparation of synthetic 5 kinds of 1 - [2 - (4 - fluorine benzene) methyl] piperazine derivatives.Conclusion:1 - [2 - (4 - fluorine benzene) methyl] piperazine derivatives worth further in-depth study. ? 引言  HYPERLINK /xz/xz7/65914xgclk.htm \t /expert/ep53/_blank 中间体?,随着哌嗪环-4 位引入不同的取代基可以产生不同的1-[二-(4- HYPERLINK /xz/xz1/2489lfluc.htm \t /expert/ep53/_blank 氟苯)甲基]-4-取代 HYPERLINK /xz/xz1/2463rfeyr.htm \t /expert/ep53/_blank 哌嗪是一类重要的 HYPERLINK /xz/xz7/63843jaorh.htm \t /expert/ep53/_blank 药物 HYPERLINK /xz/xz6/52807hxgtb.htm \t /expert/ep53/_blank 生物 HYPERLINK /xz/xz3/27359ybjbn.htm \t /expert/ep53/_blank 活性?,如治疗偏头痛药物 HYPERLINK /xz/xz4/32403rllxg.htm \t /expert/ep53/_blank 氟桂利嗪、洛美利嗪 , HYPERLINK /xz/xz2/19929dorjh.htm \t /