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Design and Synthesis of Two Indol-Steroid Derivatives

机译:两种吲哚类固醇衍生物的设计与合成

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摘要

In this study two new indol-steroid derivatives were synthesized. The first stage involves the synthesis of 17-(2-amino-thiazol-5-yl)-10, 13-dimethyl-1,2-6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-cyclopenta[a]phenanfhren-3-one (3) by the reaction of progesterone with thiourea using h as catalyst. The second stage was achieved by reaction of a brucine derivative with the compound 3 to form the compound N-(2,3-dimethoxystrychnidin- 10-ylenamino)-N'-[10, 13-dimethyl-17(2-amino-thiazol-5-yl)-1,2,6,7,8,9,10,l 1,12,13,14,15,16,17-tetradecahydro-cyclopenta-[a]phenanthren-3-ylidene]-ethane-l,2-diamine using boric acid as catalyst. The third stage was achieved by reaction of compound 3 with brucine to form 10,13-dimethyl-17-[2-(2,3-dimethoxy-strychnidin-10-ylideneamino)-thiazol-5-yl]-1,2.6,7,8,9,10,ll,12,13,14,15,16,17-tetradecahydro-cyclopenta[a]phenanthren-3-onausing boric acid as catalyst. The structure of compounds obtained was confirmed by spectrometry data.
机译:在这项研究中,合成了两种新的吲哚类固醇衍生物。第一阶段涉及17-(2-氨基噻唑-5-基)-10,13-二甲基-1,2-6,7,8,9,10,11,12,13,14,15的合成通过使用h作为催化剂的黄体酮与硫脲的反应,得到16,17-十四氢-环戊[a]苯并菲-3-酮(3)。第二阶段是通过使粗麻黄素衍生物与化合物3反应形成化合物N-(2,3-二甲氧基金丝菌素-10-亚氨基氨基)-N'-[10,13-二甲基-17(2-氨基-噻唑) -5-基)-1,2,6,7,8,9,10,l 1,12,13,14,15,16,17-十四氢-环戊-[a]菲-3-基亚基]-乙烷-1,2-二胺,以硼酸为催化剂。第三阶段是通过化合物3与马钱子碱反应形成10,13-二甲基-17- [2-(2,3-二甲氧基-施替尼丁-10-亚甲基氨基)-噻唑-5-基] -1,2.6, 7,8,9,10,11,12,13,14,15,16,17-十四氢-环戊[a]菲蒽-3-无硼酸作为催化剂。所得化合物的结构通过光谱数据确认。

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