An efficient, concise, and green visible-light-mediated [3 + 2] cycloaddition reaction for the diastereoselective synthesis of naphtho[2,3-b]furan-4,9-diones starting from readily available 2‑hydroxy-1,4-naphthoquinones and alkynes in the absence of any bases, metals, ligands, or other catalysts is described. The products could be obtained under blue LED (460 nm) irradiation at ambient temperature in 6 h with perfect regioselectivity and remarkable functional group tolerance. This approach provides an original, powerful, green, efficient, and facile way to expand the structural diversity of compounds with the structure motifs of naphtho[2,3-b]furan-4,9-diones and dihydronaphtho[2,3-b]furan-4,9-diones as promising scaffolds for novel drug discovery.

一种高效、简洁、绿色的可见光介导的[3 + 2]环加成反应，用于从容易获得的2-羟基-1,4开始非对映选择性合成萘并[2,3-b]呋喃-4,9-二酮描述了在不存在任何碱、金属、配体或其他催化剂的情况下的萘醌和炔烃。室温下在蓝色LED（460 nm）照射下6 h即可获得产物，具有完美的区域选择性和显着的官能团耐受性。该方法提供了一种新颖、强大、绿色、高效、简便的方法来扩展具有萘并[2,3-b]呋喃-4,9-二酮和二氢萘并[2,3- b ]结构基序的化合物的结构多样性。 ]呋喃-4,9-二酮作为新药发现的有前途的支架。