Perfluoroalkyl indolizine derivative and synthesis method thereof

全氟烷基吲嗪衍生物及其合成方法

Abstract

The invention relates to a perfluoroalkyl indolizine derivative and a synthesis method thereof. A structural formula of the perfluoroalkyl indolizine derivative is as shown in the specification, wherein R1 refers to H, CH3 and CO2Me; R2 refers to hydrogen, chlorine, methoxyl, nitryl or methyl; RF refers to C1-C3 perfluoroalkyl. Easily acquirable pyridine derivatives, w-bromoacetophenone derivatives and perfluoroalkyl methyl propiolate mature in synthesis technique are adopted as raw materials for one-pot synthesis of the perfluoroalkyl indolizine derivative step by step. The perfluoroalkyl methyl propiolate used as the raw materials is subjected to Michael addition under certain conditions to obtain the perfluoroalkyl indolizine derivative, operations are greatly simplified, and high atom economy and environment friendliness are realized; due to adoption of acetonitrile as a solvent, low environment pollution is realized; high regioselectivity and high yield are achieved. Therefore, the synthesis method is a novel effective method for synthesis of the perfluoroalkyl indolizine derivative.
本发明涉及一种全氟烷基吲嗪衍生物及其合成方法,该衍生物的结构式为:;其中,R1为H、CH3、CO2Me;所述的R2为氢、氯、甲氧基、硝基或甲基;所述的RF为C1~C3的全氟烷基。本发明方法以易得的吡啶衍生物、w‑溴代苯乙酮衍生物及合成手法成熟的全氟烷基丙炔酸甲酯作为原料,三组分分步一锅法合成含全氟烷基吲嗪衍生物,利用全氟烷基丙炔酸甲酯为原料,一定条件下进行Michael加成,得到全氟烷基吲嗪衍生物,操作大大简化,原子经济性高,绿色环保。反应采用乙腈作溶剂,对环境污染小。区域选择性高,产率良好。因此本方法是合成含全氟烷基吲嗪衍生物的有效新方法。

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