冬凌草甲素葡萄糖苷的合成

Synthesis of Oridonin Glucopyranoside

为研究冬凌草甲素的构效关系,合成生物活性更高的化合物,以冬凌草甲素为先导化合物,通过对其进行选择性保护,再进行糖苷化,最后脱保护,经五步反应,以23.0%的总收率,合成了冬凌草甲素-6-O-β-D-葡萄糖苷,并得到一系列冬凌草甲素衍生物,它们的结构经IR,HNMR,MS和元素分析确证.

In order to study the structure-activity relationship of oridonin derivatives, the target compound oridonin-6-O-beta-D-glucopyranoside was synthesized from oridonin and tetra-O-benzoyl-alpha-D-glucopyranosyl bromide via protection, Koenigs-Knorr reaction and deprotection in the total yield of 23.0%. The structures of the oridonin derivatives were confirmed by IR, H-1 NMR, MS spectra and elemental analysis.