Erianin, a low-molecular-weight natural product isolated from dendrobium, has demonstrated significant anti- tumor activity in numerous in vitro cytotoxicity experiments. As a result, its efficient synthesis has garnered considerable attention from chemists and pharmacologists. However, previously reported synthetic routes for Erianin are cumbersome and require harsh reaction conditions, rendering them unsuitable for large-scale industrial applications. This article mainly introduces a novel synthetic method for Erianin with a total yield of 49% (4 steps), featuring the construction of the core diphenyl acetylene motif via the classic Sonogashira coupling reaction, followed by catalytic hydrogenation. The new procedure enjoys mild reaction conditions, short synthetic steps, operational simplicity, and high efficiency.

Key words: Erianin, synthetic route, Sonogashira coupling, bioactive