Benzofuran and 2,3-dihydrobenzofuran scaffolds are core components in a large number of biologically active natural and synthetic compounds including approved drugs. Herein, we report efficient synthetic protocols for preparation of libraries based on 3-carboxy 2-aryl benzofuran and 3-carboxy 2-aryl trans-2,3-dihydrobenzofuran scaffolds using commercially available salicylaldehydes, aryl boronic acids or halides and primary or secondary amines. The building blocks were selected to achieve variation in physicochemical properties and statistical molecular design and subsequent synthesis resulted in 54 lead-like compounds with molecular weights of 299-421 and calculated octanol/water partition coefficients of 1.9-4.7.

中文翻译：

---

基于苯并呋喃和2,3-二氢苯并呋喃支架的面向多样性的图书馆合成。

苯并呋喃和2,3-二氢苯并呋喃支架是包括批准药物在内的许多具有生物活性的天然和合成化合物的核心成分。在此，我们报告了使用可商购的水杨醛，芳基硼酸或卤化物以及伯胺或仲胺，基于3-羧基2-芳基苯并呋喃和3-羧基2-芳基反式2,3-二氢苯并呋喃骨架制备文库的有效合成方案。 。选择结构单元以实现理化性质和统计分子设计的变化，随后的合成产生了54种铅样化合物，分子量为299-421，计算出的辛醇/水分配系数为1.9-4.7。