Synthesis of 25-hydroxycholesterol from bisnoralcohol

25-Hydroxycholesterol not only exhibits various important biological activities but also plays a crucial role in the synthesis of 25-hydroxyvitamin D₃. To date, researchers have proposed multiple synthetic routes for 25-hydroxycholesterol. Herein, a novel synthetic method for 25-hydroxycholesterol is described, involving a seven-step reaction that starts from economical and commercially available plant-derived bisnoralcohol, with an overall yield of up to 43.4%. Key reaction conditions, including solvents, reaction temperatures, bases and catalysts, were thoroughly investigated and optimized. This novel synthetic route provides a cost-effective strategy for the potential large-scale production of plant-derived 25-hydroxycholesterol.