64109-72-4

Compounds having the structure, their salts or N-oxide derivatives: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.

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As part of our program to develop estrogenic radioligands for use in nuclear medicine, a study was undertaken to investigate the effect of substituents on the receptor affinity of putative radiochemicals.In the study a synthetic strategy directed toward the introduction of an 11β-(fluoroethyl) substituent was devised.The target compound 9 was prepared via a five-step procedure starting from 11β-vinylestrone 3-acetate (4) in an overall 43percent yield.The final product and several analogues, 11β-ethyl-, -vinyl-, and (hydroxyethyl)estradiols (11, 5, and 12), were evaluated for their estrogen receptor binding affinity.The results indicate that the target compound and several 11β-substituted analogues possess relative binding affinities greater than of estradiol and its 16α-fluorinated derivatives.The manner in which the target compound 9 was prepared is amenable to use with 18F incorporation.