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目的 研究曲格列酮的合成路线。方法 为避免选择性醚化反应,将前两步(还原和选择性醚化)反应,重新设计和调整为三步反应,即酯化、醚化和还原反应。结果 每步反应专属性较强。有二个新的化合物(Ⅱ)和(Ⅲ)生成;整个反应革除了用柱色谱分离而直接得到产物。结论 酚醚化反应收率为98%,比文献报道提高了10%以上。总收率约为17%,并有工业化生产的可能。
Objective To study the synthetic route of troglitazone. Methods To avoid selective etherification, the first two steps (reduction and selective etherification) were redesigned and adjusted to three-step reactions, ie esterification, etherification and reduction. The results of each reaction is more specific. Two new compounds (II) and (III) were formed; the entire reaction was obtained directly without isolation by column chromatography. Conclusion The yield of phenol etherification is 98%, which is 10% higher than that reported in the literature. The total yield of about 17%, and the possibility of industrial production.