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研究发现新型四氢咔唑衍生物ZG02有较强的体内外降糖与降脂活性,是一个有深入开发价值的候选化合物。前期报道的制备方法存在总产率低、纯化困难等问题。本研究经方法改进后以4-氧代环己基甲酸为原料,经烯丙基保护、Fischer-吲哚环合、酰化及脱保护等4步反应得到目标产物,总收率为71.9%。同时,利用手性制备柱对ZG02进行了拆分,得到了光学纯异构体,以便进一步评价不同构型异构体的生物活性差异。
The study found that the new tetrahydrocarbazole derivative ZG02 has strong in vivo hypoglycemic and lipid-lowering activity, is a candidate for further development of the value of the compound. The preparation method reported in earlier period has the problems of low total yield, difficult purification and the like. In this study, 4-oxocyclohexylcarboxylic acid was used as the starting material after the method was improved, and the target product was obtained by allyl protection, Fischer-Indole cyclization, acylation and deprotection. The total yield was 71.9%. At the same time, ZG02 was resolved by chiral preparative column, and optical pure isomers were obtained in order to further evaluate the biological activity difference of different configurational isomers.