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本文系叙述甾体药物中各种具有生理活性基团的引入方法。近年来由于有机合成方法的发展,某些甾体药物已可得之于全合成,本文将加以讨论。现分述如下。 1.加入1,4-双烯: 微生物可使A环饱和的5α-3-酮化合物的A环脱氢,如镰刀菌(Fusarium)使雄甾-5α-3,17-双酮脱氢生成 1,4-双烯;节杆菌可使16β-甲基-5α-双氢可的松脱氢形成 1,4-双烯,得率46％。节杆菌使西△~(9(11))-16β-甲基-5α-孕甾-17α,21-双羟基-3,20-双酮-21-乙酸酯(Ⅰ)脱氢时,同时在△~(9(11))引入α-环氧。若用节杆菌和诺卡氏菌(Nocardia sp.)两种菌混合培养则主要获得1,4-脱氢产物(Ⅱ),产率50％,少量是9α,11α-环氧化合物(Ⅲ)。Ⅱ是合
This article describes the introduction of various physiologically active groups in steroidal drugs. In recent years due to the development of organic synthesis methods, some of the steroid drugs have been available in the total synthesis, which will be discussed in this article. Now is as follows. 1. Addition of 1,4-diene: The microorganism can dehydrogenate the A ring of the A-ring-saturated 5α-3-keto compound, such as Fusarium dehydrogenation of androsta-5α-3,17- 1,4-diolefin; Arthrobacter can dehydrogenate 16β-methyl-5α-dihydrocortisone to form 1,4-diolefin in 46% yield. When Arthrobacter was dehydrogenated, western △ ~ (9 (11)) - 16β-methyl-5α-pregna-17α, 21-bishydroxy-3,20-dione-21-acetate Α-Epoxy was introduced at Δ ~ (9 (11)). If the mixture of Arthrobacter and Nocardia sp. Is used, the 1,4-dehydrogenation product (II) is mainly obtained in a yield of 50% and a small amount of 9α, 11α-epoxy compound (III) . Ⅱ is combined