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A New Method for Preparation of 19 nor steroids substituted in position 2

机译:一种制备19位或2位取代的类固醇的新方法

摘要

Process for the production of 19 nor steroids substituted in position 2, of formula (i), wherein R1, R2, R3 and R4 may be several types of radicals.Submits to the vittig condensation reaction of a compound of formula (ii), in which K And K '' represent a Keto Group locked in the form of ketal, and R3 is a radical alcohilo 2 to 4 carbon ATOMS, with a trifenilfosfonio Halide in the presence of a strong base. The resulting product was hidrobora, oxidized in Alkaline medium, and ciclisa deacetylating.Blocking the function of the product obtained in the form of alcohol ether and treated with halide alcohilo, alquenilo or aluinilo in Basic Medium. Hydrolyzed and oxidized. Halogen is in position and acetoxila 21 and, eventually, foam. Is treated with an Acid, an Acid Functional derivative containing 1 to 20 carbon ATOMS, or a functional Derivative of Phosphoric acid.These compounds have pharmacological application in the treatment of hypertension and heart failure. * L * formula
机译:制备19个在式(i)的位置2上取代的甾族化合物的方法,其中R1,R2,R3和R4可以是几种自由基。进行式(ii)化合物的vittig缩合反应,其中K和K''代表以缩酮形式锁定的Keto基团,R3为自由基的2至4个碳原子的ATOMS,在强碱的存在下带有trifenilfosfonio卤化物。所得产物是hidrobora,在碱性介质中被氧化,并且ciclisa脱乙酰基。阻止了以醇醚形式获得的产物的功能,并在碱性介质中用卤化物alcohilo,alquenilo或aluinilo处理。水解和氧化。卤素就位,乙酰氧基21并最终起泡沫。用酸,含有1至20个碳原子的ATOMS的酸功能衍生物或磷酸的功能衍生物进行治疗。这些化合物在高血压和心力衰竭的治疗中具有药理应用。 * L *公式

著录项

  • 公开/公告号ES8102149A1

    专利类型

  • 公开/公告日1981-04-01

    原文格式PDF

  • 申请/专利权人 ROUSSEL-UCLAF;

    申请/专利号ES19790486791

  • 发明设计人

    申请日1979-12-12

  • 分类号C07J5/00;A61K31/57;

  • 国家 ES

  • 入库时间 2022-08-22 15:49:30

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