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A method for the production of steroid - carb oxalates

机译:一种生产类固醇-草酸酯的方法

摘要

PURPOSE:To obtain the title compound useful as an intermediate for diuretics industially advantageously, by reacting an alkali metal salt of 17beta-hydroxypregnen- 20-yn-3-one 3-acetal with carbon dioxide, followed by hydrolysis. CONSTITUTION:A 17beta-hydroxypregnen-20-yn-3-one-3-acetal shown by the formula I (Z is 1-10C alkylene) is reacted with a dimusyl alkali metal shown by the formula II (M is alkali metal) in a solvent, e.g., tetrahydrofuran, etc. to give a compound shown by the formula III, which is cooled to -20 deg.C and reacted with carbon dioxide bubbled into the solution to give a 3-(17beta-hydroxyandrostene-3-one 3-acetal- 17alpha-yl)propiolate shown by the formula IV. This compound is hydrolyzed to give the desired carboxylic acid. USE:A raw material for producing an anti-androsterone diuretic and a hypotensor.
机译:目的:通过将17β-羟基孕烯-20-yn-3-one 3-缩醛的碱金属盐与二氧化碳反应,然后进行水解,以有利地获得工业上用作利尿剂中间体的标题化合物。组成:使式Ⅰ所示的17β-羟基孕烯-20-yn-3-酮-3-缩醛(Z为1-10C亚烷基)与式Ⅱ所示的二甲基碱金属(M为碱金属)反应。用溶剂,例如四氢呋喃等得到式Ⅲ所示的化合物,将其冷却至-20℃,并与鼓入溶液中的二氧化碳反应,得到3-(17β-羟基雄烯-3-式IV所示的3-缩醛-17α-基)丙酸酯。将该化合物水解,得到所需的羧酸。用途:生产抗雄甾酮利尿剂和降压药的原料。

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