【药物名称】RU 16117
化学结构式(Chemical Structure):
参考文献No.50797
标题:RU-16117
作者:Azadian-Boulanger, G.; Raynaud, J.P.
来源:Drugs Fut 1985,10(5),926
合成路线图解说明:

RU-16117 is synthesized from D9(11)-estradiol (I). After protecting the hydroxyl groups by the formation of a benzyl ether (II), the double bond is hydrated by hydroboration, followed by oxidation with hydrogen peroxide in alkali. The alcohol thus formed (III) is treated with sodium hydride and then methyliodide (IV). After deprotection of the 3 and 17 hydroxyl groups (V), the C-17 hydroxyl is oxidized to a ketone by chromic oxidation (VI) and the 17-alpha-ethynyl group is introduced directly with potassium acetylide.

参考文献No.700641
标题:Analyse Radiocristallographique de Mol閏ules Oestrog鑞es et Androg鑞es et Etude de leur Affinit?et de leur Sp閏ificit?
作者:Pr閏igous, G.
来源:Ph. D. Thesis, Univ. Bordeaux I 1978,
合成路线图解说明:

RU-16117 is synthesized from D9(11)-estradiol (I). After protecting the hydroxyl groups by the formation of a benzyl ether (II), the double bond is hydrated by hydroboration, followed by oxidation with hydrogen peroxide in alkali. The alcohol thus formed (III) is treated with sodium hydride and then methyliodide (IV). After deprotection of the 3 and 17 hydroxyl groups (V), the C-17 hydroxyl is oxidized to a ketone by chromic oxidation (VI) and the 17-alpha-ethynyl group is introduced directly with potassium acetylide.

参考文献No.800056
标题:D閞iv閟 11-alpha-m閠hoxyl閟 de l'estradiol: Activit?anti-estrog鑞e du 11-alpha-m閠hoxy 閠hynyl estradiol: RU-16117
作者:Bouton, M.M.; Raynaud, J.P.; Azadian-Boulanger, G.; Bucourt, .; Pierdet, A.; Torelli, V.; N閐閘ec, L.
来源:Eur J Med Chem 1978,13(4),313-319
合成路线图解说明:

RU-16117 is synthesized from D9(11)-estradiol (I). After protecting the hydroxyl groups by the formation of a benzyl ether (II), the double bond is hydrated by hydroboration, followed by oxidation with hydrogen peroxide in alkali. The alcohol thus formed (III) is treated with sodium hydride and then methyliodide (IV). After deprotection of the 3 and 17 hydroxyl groups (V), the C-17 hydroxyl is oxidized to a ketone by chromic oxidation (VI) and the 17-alpha-ethynyl group is introduced directly with potassium acetylide.

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