目的 尋找一條合成目標(biāo)化合物4-(6-脫氧-β-D-吡喃葡萄糖基)-1-甲氧基-2-[(反式-4-正丙基環(huán)己基)甲基]苯的簡(jiǎn)易路線，并研究其晶型。方法 利用苯基溴化物片段和6-脫氧葡萄糖酸內(nèi)酯片段作為起始原料合成目標(biāo)化合物；采用有機(jī)混合溶劑和含水混合溶劑結(jié)晶的方式制備目標(biāo)化合物的晶型，采用粉末X射線衍射分析和熱重–差熱分析技術(shù)對(duì)其進(jìn)行表征，并對(duì)其進(jìn)行了初步穩(wěn)定性研究。結(jié)果 目標(biāo)化合物的總收率為74%，通過(guò)上述制備方法獲得了同一種晶型，該晶型對(duì)光、熱和濕均是穩(wěn)定的。結(jié)論 設(shè)計(jì)了一條合成目標(biāo)化合物的簡(jiǎn)易路線，該路線操作簡(jiǎn)便、路線短、收率高，并制備了一種具有良好穩(wěn)定性的目標(biāo)化合物的晶型。

Objective To search for a facile synthetic route for synthesis of target compound 4-(6-deoxy-β-D-glucopyranosyl)-1- methosyl-2-[(trans-4-n-propylcyclohexyl)methyl] benzene and to study its polymorphic characteristics. Methods A phenyl bromide fragment and 6-deoxygluconolactone fragment were used as starting materials to synthesize the target compound. Polymorph of target compound was prepared from organic mixed solvents and aqueous mixed solvents. and was characterized by powder X ray diffraction (PXRD), and thermogravimetric analysis coupled with differential thermal analysis (TG-DTA), and the preliminary stability properties of the polymorph was also studied. Results The total yield of target compound was 74%. The same polymorph of the target compound was obtained by the above methods, and was stable to light, heat, and moisture. Conclusion A facile synthetic route for synthesis of target compound is developed, which has the advantages of simple operating procedure, easy post-processing and high yield, and a stable polymorph of target compound is obtained.

國(guó)家自然科學(xué)基金資助項(xiàng)目（21302141）；天津市科技計(jì)劃項(xiàng)目（10ZCKFSH01300）