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脱氧可的松置于1,4-二氧六环,Sodium Bismuthate,硫酸,对甲苯磺酸体系中,化学反应生成3-氧代-雄甾-4-烯-17Beta-羧酸
参考文献:Tsuda Et Al.,Chemical And Pharmaceutical Bulletin,1959,Vol. 7,P. 519,521
标题:Tsuda Et Al.,Chemical And Pharmaceutical Bulletin,1959,Vol. 7,P. 519,521

专利信息

专利号:WO-2013001322-A1
优先权日:2011-06-30
标 题:PROCESS FOR THE SYNTHESIS OF (5α,17β)-N-[(2,5-BIS(TRIFLUOROMETHYL)-PHENYL]-3-OXO-4-AZA-5-ANDROST-1-ENE-17-CARBOXAMIDE
发明人：SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES
权利人:RICHTER GEDEON NYRT; SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES
摘要:The synthesis consists of reaction steps as follows: oxidizing the α,β-unsaturated ketone system of ring 'A' of pregn-4-ene-3,20-dion- of formula (II) with sodium metaperiodate in tert-butanol in the presence of potassium permanganate and alkali metal carbonate, reacting the obtained 3,5-seco acid with an ester of chloroformic acid in the presence of tertier organic base below 0°C, reacting the obtained new compound after isolation or without isolation with ammonia or ammonium acetate, cyclization of the resulting carboxamides with an acid, cathalytic hydrogenating the obtained ene lactame, and oxidizing the side chain at position 17 of the obtained pregnane compound with an alkali metal hypobromide in aqueous dioxane below 10°C. Thereafter on one hand the obtained (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is reacted with chloroformic acid ester, the obtained new compound is reacted with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acid, the obtained amide is reacted with trimethyl chlorosilane in inert atmosphere in the presence of Î?,Î?,Î?',Î?'-tetramethyl-ethylendiamine, then en excess iodine is added to the reaction mixture and the product of the iodination reaction is crystallized from acetonitrile, then the obtained 2-iodo-3-oxo-4-aza-17β-carboxamide is reacted with potassium tert-butylate to furnish final product. On the other hand, (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is transformed into methylester by known method, this latter is transformed into methyl (2α,5α,17β)-2-iodo-3-oxo-4-aza-5-androstane-17-carboxylate according to known method, the obtained compound is reacted with potassium-tert-butylate, the obtained (5α,17β)-3-oxo-4-aza-5-androst-1-ene-17-carboxylic acid is reacted with an ester of chloroformic acid, then the obtained new compound is coupled with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acidcatalyst to gain final product.