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甾体17β-羧酰胺衍生物的合成

Synthesis of steroidal 17 beta-carboxamide derivatives.

作者信息

Formstecher P, Lustenberger P, Dautrevaux M

出版信息

Steroids. 1980 Mar;35(3):265-71. doi: 10.1016/0039-128x(80)90039-2.

Abstract

Several 17 beta-carboxamide derivatives of natural and fluorinated glucocorticoids have been synthesized. The 17 beta-carboxylic derivatives were obtained by periodic acid oxidation of their side chains. They were then activated by N-hydroxybenzotriazole (HOBT) and coupled to several primary amines. Using this method eleven 17 beta-carboxamide derivatives have been prepared in good yields.

摘要

已经合成了几种天然和氟化糖皮质激素的17β-羧酰胺衍生物。17β-羧酸衍生物通过其侧链的高碘酸氧化获得。然后它们用N-羟基苯并三唑(HOBT)活化并与几种伯胺偶联。使用这种方法,以良好的产率制备了11种17β-羧酰胺衍生物。

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