Osteoporosis is a system in which the microstructure of the bone tissue is damaged, the bone mineral composition and the bone matrix are continuously reduced, the bone is thinned, the number of trabecular bone is reduced, the bone fragility is increased, and the fracture risk is increased. A disease of bone metabolism disorder. Generally divided into two categories, primary osteoporosis and secondary osteoporosis.
Foreign statistics show that there are about 200 million people suffering from osteoporosis worldwide, including more than 75 million in the United States, Western Europe and Japan alone. Osteoporosis is recognized as the second-largest health killer after cardiovascular disease. Driven by demand, a market of tens of billions of dollars has been formed. The cost of treatment and hospitalization is as high as $25 billion a year. In the United States alone, the cost of osteoporosis-related medical care (including hospitalization and home care) reached $17 billion in 2001, or about 47 million a day. Dollar. This number is still rising.
There are 84 million people with osteoporosis (including bone loss) in China, accounting for 6.6% of the total population. It is estimated that by 2010, the number of potential osteoporosis patients will increase to 114 million; in 2025, 150 million people will be reached. . Due to the influence of osteoporosis, the incidence of hip fracture in elderly people over 50 years old is 11.26/100,000 in southern cities, 74.6/100,000 in northern areas, and the average age of onset of hip fractures is 67.2 years. Osteoporosis is a major cause of fracture in the elderly. Osteoporosis, which has long been considered a disease of the elderly in our country, actually existed in childhood. It is particularly important to note that there is currently no safe and effective cure in medicine to help the loose bones return to their original state. Therefore, it is particularly important to recognize and prevent early prevention.
In order to solve the above technical problems, the present invention discloses a process for preparing high-purity minodronic acid, which is simple in operation, and the high-purity minodronic acid produced by the process can effectively treat osteoporosis and avoid hip fracture and the like. Major diseases.
The following process steps are included: First, Ethyl trans-4-oxo-2-butenoate CAS 2960-66-9 is used as a raw material to form a ring with 2-aminopyridine to form 2‐(imidazo[1,2‐a]‐3‐ Ethyl acetate, and then hydrolyzed to obtain 2 -(imidazo[1,2-a]-3-yl)acetic acid; then, 2 -(imidazo[1,2-a]-3-yl)acetic acid The crude product of minodronic acid is prepared by reacting with phosphorous acid and phosphorus trichloride; finally, the crude minodronic acid is refined by hydrochloric acid to obtain a finished product. The high-purity minodronic acid produced by this process can effectively treat osteoporosis and avoid major diseases such as hip fracture.