An efficient solid-phase synthetic route for the construction of 1,3,4-oxadiazole and 1,3,4-thiadiazole libraries based on branching diversity-oriented synthesis (DOS) has been developed in this study. The core skeleton resins, 1,3,4-oxadiazole and 1,3,4-thiadiazole, were obtained through desulfurative and dehydrative cyclizations of thiosemicarbazide resin, respectively. Various functional groups have been introduced to the core skeleton resins, such as aryl, amine, amide, urea, thiourea, and an amino acid. Most of the libraries were purified by simple trituration without extraction or column chromatography after cleavage of the products from the solid-supported resin. As a result, we obtained high yields of pure 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives (total numbers = 128). Finally, we confirmed the drug-like properties of our library by calculation of physicochemical properties, displays of the skeletal diversities of the library in 3D-space, and occupation of a broad range of areas by their functional groups.

中文翻译：

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基于固相支持物支化多样性导向合成的具有高水平骨架多样性的1,3,4-恶二唑和1,3,4-噻二唑文库的构建

在这项研究中，开发了一种有效的固相合成路线，该路线基于分支多样性定向合成（DOS）构建1,3,4-恶二唑和1,3,4-噻二唑库。核心骨架树脂1,3,4-恶二唑和1,3,4-噻二唑分别通过硫代氨基脲树脂的脱硫和脱水环化获得。各种官能团已经引入到核心骨架树脂中，例如芳基，胺，酰胺，脲，硫脲和氨基酸。从固相支持的树脂上裂解产物后，大多数文库通过简单的研磨纯化而无需萃取或柱色谱法。结果，我们获得了高产率的纯1,3,4-恶二唑和1,3,4-噻二唑衍生物（总数= 128）。最后，