Hydroxyl ferrocene is an important intermediate for the synthesis of ferrocene derivatives. There are several methods for the synthesis of 1-ferrocenylethanol whereas the synthesis of 2-ferrocenylethanol is rarely reported. In this work, the target compound 2-ferrocenylethanol was synthesized through a three-step reaction: first, acetyl ferrocene was prepared from ferrocene and acetic anhydride by Friedel-Grafts acylation reaction, then ferrocenylacetic acid was synthesized by Willgerodt-Kindler reaction, followed 2-ferrocene ethanol was obtained by reduction reaction. The effects of different reaction conditions on the yield of 2-ferrocenylethanol from ferrocenylacetic acid were studied. The optimum reduction conditions were determined as follows: the reducing agent was lithium aluminum hydride; n (lithium aluminum hydride): n (ferrocenylacetic acid) was 8 : 1; the solvent was tetrahydrofuran; the reaction temperature was 25C; the reaction time was 24 h, and the yield of 2-ferrocenylethanol was 82 %. Subsequently, anti-tumor activities of 2-ferrocenylethanol were evaluated against human breast cancer MCF-7 and MDA-MB-231, human liver cancer HepG2, human cervical cancer HeLa cell lines in vitro. The preliminary activity test results showed that 2-ferrocenylethanol showed obvious inhibitory activities, against MCF-7, MDA-MB-231, HepG2 and HeLa, and its half inhibitory concentration (IC50) value was 17.4, 12.9, 20.7, 24.6 μmol/L, respectively. Additionally, 2-ferrocenylethanol was nontoxic to normal MCF-10A cells, while the positive control drug 5- FU exhibited essential toxicity.