【药物名称】F-17alpha-CH3-DHT
化学结构式(Chemical Structure):
参考文献No.543390
标题:7alpha-Iodo and 7alpha-fluoro steroids as androgen receptor-mediated imaging agents
作者:Labaree, D.C.; Hoyte, R.M.; Nazareth, L.V.; Weigel, N.L.; Hochberg, R.B.
来源:J Med Chem 1999,42(11),2021
合成路线图解说明:

Ketalization of 17alpha-methyltestosterone (I) by means of ethylene glycol and p-toluenesulfonic acid provided the DELTA5(6)-ketal (II), and subsequent allylic oxidation of (II) with CrO3-3,5-dimethylpyrazole complex gave enone (III). Hydrogenation of the olefinic double bond of (III) afforded the saturated ketone (IV), which was reduced employing NaBH4 and CeCl3 to furnish an unseparable mixture of epimeric alcohols (Va-b). After removal of the ethylene ketal of (Va-b) with p-toluenesulfonic acid/acetone, the major 7beta-alcohol (VI) was isolated by flash chromatography. The 7beta-tosylate (VII) was then prepared by reaction of (VI) with p-tosyl chloride in pyridine. Finally, exchange of the tosylate group of (VII) with tetrabutylammonium fluoride yielded the desired 7alpha-fluoride.

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