首页> 外国专利> 16 + 17 - acetal - substituted androstane - 17 - beta - carbonsaeureester, procedures to their manufacture and pharmaceutical praeparate containing them.

16 + 17 - acetal - substituted androstane - 17 - beta - carbonsaeureester, procedures to their manufacture and pharmaceutical praeparate containing them.

机译:16 + 17-缩醛取代的雄烷-17-β-碳磺脲酸酯,其生产程序以及含有它们的药用普萘酸盐。

摘要

The invention relates to the preparation of a compound of the formula CHEM or a stereoisomeric compound thereof, in which formula the the l,2-position is saturated or is a double bond; X1 is selected from hydrogen, fluorine, chlorine and bromine X2 is selected from hydrogen, fluorine, chlorine and bromine R2 is selected from straight and branched hydrocarbon chains having l-l0 carbon atoms and R7 is hydrogen or an acyl group with l-l0 carbon atoms arranged in a straight or branched chain, characterized by reaction of a steroid compound of the formula CHEM with an aldehyde compound of the formula CHEM wherein X1, X2, R2, R7 and IMAGE have the meanings given above, in the presence of an acid catalyst. The products of the process are useful intermediates in the preparation of novel glucocorticosteroids which possess high anti-inflammatory potency at the place of application and low glucocorticord systemic potency.
机译:本发明涉及式的化合物或其立体异构化合物的制备,其中式I,2-位为饱和或为双键; X 1选自氢,氟,氯和溴X 2选自氢,氟,氯和溴R 2选自具有1-10个碳原子的直链和支链烃链,R 7为氢或具有1-10个碳的酰基排列成直链或支链的原子,其特征在于式的类固醇化合物与式的醛化合物反应,其中X1,X2,R2,R7和具有上述含义,在酸催化剂的存在下。该方法的产物是用于制备新型糖皮质类固醇的有用的中间体,所述新型糖皮质类固醇在应用场所具有高的消炎效力和低的糖皮质激素全身效力。

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