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As a systemic metabolic disease caused by a variety of factors, osteoporosis is characterized by reduced bone mass, bone tissue microstructural degradation, and decreased bone mechanical properties, accompanied by bone fragility and fracture, which is a common risk of senile disease. In China, osteoporosis has become a common disease and has frequent morbidity, with the incidence trend on the rise. Bisphosphates have received much attention in this field as inhibitory bone resorption agents, and sodium olpadronate belongs to the third-generation bisphosphonates. This experiment investigated the synthetic process and pharmacological activity of sodium olpadronate. Using 3-(N,N-dimethylamino)-propionitrile as the starting material, the synthesis process was improved to reduce cost with a total yield of 49.7%, which was 24.0% higher than that reported in the literature. Pharmacodynamic experiments showed that sodium olpadronate could be used to treat osteoporosis. Moreover, toxicology experiments showed no obvious toxic side effects. Taken together, sodium olpadronate had very promising development prospects. [ABSTRACT FROM AUTHOR]