盐酸吡格列酮的合成工艺研究

Research on Pioglitazone Hydrochloride Synthesis Process

本文以如下合成路线为基础:羟基苯甲醛与2,4-噻唑烷二酮缩合后,经催化氢化,再与2-羟乙基-5-乙基吡啶磺酸酯对接,成盐得到盐酸吡格列酮,然后考察了催化氢化步骤中催化剂种类、用量、溶剂种类、反应温度和反应时间对反应收率的影响,从而找到了最适宜的催化氢化的反应工艺参数:催化剂为雷尼镍,催化剂用量为雷尼镍与中间体(5)的质量比为80%,溶剂为甲醇,反应温度为105℃,反应时间5h。找到了一个既能提高反应的收率,而且经济适用,适合工业化大生产的反应工艺。

In this paper, based on the following synthetic route： hydroxy benzaldehyde and 2, 4 - Margaret diketone condensation, through catalytic hydrogenation, with 2 - hydroxyethyl ethyl pyridine - 5 - sulphonic acid ester and docking, as pioglitazone hydrochloride salt, and then examines the catalytic hydrogenation steps in the varieties and amount of the catalyst, the type of solvent, reaction temperature and reaction time influencing on the yield of reaction, so as to find the optimum catalytic hydrogenation reaction process parameters： for rainie nickel catalyst, catalyst for rainie nickel and intermediates （5） the weight ratio of 80%, for methanol solvent, reaction temperature is 105 ℃, the reaction time of 5 hours. Found an improved, affordable, suitable reaction route for industrialized production of reaction process.