首页> 外国专利> PREPARATION OF 7ALPHAAACETYLTHIOO177HYDROXYY33OXOO17ALPHAAPREGNN 44ENEE211CARBOXYLIC ACID GAMMAALACTONE

PREPARATION OF 7ALPHAAACETYLTHIOO177HYDROXYY33OXOO17ALPHAAPREGNN 44ENEE211CARBOXYLIC ACID GAMMAALACTONE

机译:制备7ALPHACEACETYLTHIOO177HYDROXYY33OXOO17ALPHAAPREGNN 44ENEE211羧酸丙内酯

摘要

PURPOSE:To prepare the titled compound useful as a diuretic, in high yield, by adding thioacetic acid to 17-hydroxy-3-oxo-17alpha-pregna-4,6-diene-21-carboxylic acid gamma- lactone in a specific solvent, and separating the addition product by crystallization. CONSTITUTION:17-Hydroxy-3-oxo-17alpha-pregna-4,6-diene-21-carboxylic acid gamma- lactone is made to react with thioacetic acid in N-methyl-2-pyrrolidone or N,N- dimethylacetamide to afford 7alpha-acetylthio-17-hydroxy-3-oxo-17alpha-pregn-4-ene-21- carboxylic acid gamma-lactone, which is then separated by crystallization. EFFECT:The production of by-product is essentially none, and the objective compound can be obtained in high purity. The purification is easy, and the economical effect is significant. The objective compound is prepared in high purity at a stoichiometric yield even by using crude, low-purity raw materials.
机译:目的:通过在特定溶剂中将硫代乙酸添加到17-羟基-3-氧代-17α-孕烯-4,6-二烯-21-羧酸γ-内酯中,以高收率制备标题化合物,用作利尿剂,并通过结晶分离加成产物。组成:使17-羟基-3-氧代17α-孕烯-4,6-二烯-21-羧酸γ-内酯与硫代乙酸在N-甲基-2-吡咯烷酮或N,N-二甲基乙酰胺中反应,得到7α-乙酰硫基-17-羟基-3-氧代-17α-孕烯-4-烯-21-羧酸γ-内酯,然后通过结晶分离。效果:基本上不产生副产物,并且可以高纯度获得目标化合物。纯化容易,经济效果显着。即使使用粗制的低纯度原料,也可以以化学计量的收率高纯度地制备目的化合物。

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