Synthesis Of Selective Estrogen Receptor Modulators: Pipendoxifene

Osteoporosis is a systemic skeletal disease, characterized by low bone mass anddeterioration of bone tissue, with a consequent increase in bone fragility andsusceptibility to fracture . The elderly are at greatest risk of osteoporosis, and theproblem is therefore predicted to increase significantly with the aging of the population.Worldwide fracture incidence is forecast to increase three-fold over the next 60 years,.Women are at greater risk of osteoporosis than men. Women experience a sharpacceleration of bone loss during the five years following menopause. Other factors thatincrease the risk include smoking, alcohol abuse, a sedentary lifestyle and low calciumintake.Estrogen is the agent of choice in preventing osteoporosis or post menopausal boneloss in women; it is the only treatment which unequivocally reduces fractures. Long-termestrogen therapy, however, can increase the risk of uterine cancer and possibly breastcancer. Combinations of progesterone with estrogen can lessen the cancer risk, but it alsoblunts the serum cholesterol lowering effects of estrogen. Because of the disadvantagesof the estrogen, the scientists synthesized a series of compounds called selective estrogenreceptor modulaters, including Tamoxifene,raloxifene,lasoxifene,bazedoxifene,pipendoxifene and so on. They exert selective effects on different tissues in the body, itproduces estrogen-like effects on bone and the cardiovascular system while antagonizingthe detrimental effects of estrogen on uterine and breast tissue.Introduce the character of the 2-phenylindoles compounds, design a new route tosynthesize Pipendoxifene successgully, furthermore research the technics ofintermediates of Pipendoxifene.The structures of the key intermediates and the target product were confirmed bythe analysis of 1H-NMRdata.