Propofol has been widely used as a clin. anesthetic for a few decades. Its derivative with a three-membered ring, Cipepofol, was found to be equally effective and with less side effects. Here, we report a process for the scale-up total synthesis of Cipepofol. It could be obtained in five steps from the com. available 2-isopropylphenol. The key reactions involved Claisen rearrangement, Simmons-Smith cyclopropanation, and chiral resolution through carbamate formation/crystallization, followed by hydrolysis and wiped-film distillation The reaction conditions were mild, and the involved reagents were easily accessible. With this process, the final product was synthesized in a 14% overall yield, without column chromatog. purification The synthetic route offered a shorter, robust, and economical production of Cipepofol (chem. purity > 99.5%, 99.5% ee) in kg scale.