or a stereoisomeric compound thereof, in which formula the the 1,2-position is saturated or is a double bond;X1 is selected from hydrogen, fluorine, chlorine and bromineX2 is selected from hydrogen, fluorine, chlorine and bromineR2 is selected from straight and branched hydrocarbon chains having 1-10 carbon atoms andR7 is hydrogen or an acyl group with 1-10 carbon atoms arranged in a straight or branched chain, characterized by reaction of a steroid compound of the formulawith an aldehyde compound of the formulawherein X1, X2, R2, R7 andhave 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."/>
Process for the preparation of intermediates for 11-beta,16-alpha,17-alpha,21-tetrahydroxypregna-3,20-dione 16-alpha,17-alpha-acetals and 21-esters thereof
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Process for the preparation of intermediates for 11-beta,16-alpha,17-alpha,21-tetrahydroxypregna-3,20-dione 16-alpha,17-alpha-acetals and 21-esters thereof
Process for the preparation of intermediates for 11-beta,16-alpha,17-alpha,21-tetrahydroxypregna-3,20-dione 16-alpha,17-alpha-acetals and 21-esters thereof
The invention relates to the preparation of a compound of the formulaor a stereoisomeric compound thereof, in which formula the the 1,2-position is saturated or is a double bond;X1 is selected from hydrogen, fluorine, chlorine and bromineX2 is selected from hydrogen, fluorine, chlorine and bromineR2 is selected from straight and branched hydrocarbon chains having 1-10 carbon atoms andR7 is hydrogen or an acyl group with 1-10 carbon atoms arranged in a straight or branched chain, characterized by reaction of a steroid compound of the formulawith an aldehyde compound of the formulawherein X1, X2, R2, R7 andhave 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.展开▼
机译：本发明涉及下式的化合物的制备 <图像文件=“ IMGA0001.GIF” he =“ 57” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 120” /> 或其立体异构化合物，其中式1，2-位为饱和或为双键; X 1 选自氢，氟，氯和溴<！-EPO - > X 2 选自氢，氟，氯和溴 R 2 选自直链和支链烃具有1-10个碳原子且 R 7 的链是氢或具有1-10个碳原子的直链或支链排列的酰基，其特征在于类固醇的反应式的化合物 <图像文件=“ IMGA0002.GIF” he =“ 65” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 109” /> 与下式的醛化合物 <图像文件=“ IMGA0003.GIF” he =“ 22” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 32” /> ，其中X 1 ，X 2 ，R 2 ，R 7 和 <图像文件=“ IMGA0004.GIF” he =“ 10” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 35” /> 在酸催化剂的存在下，具有以上给出的含义。该方法的产物是制备新型糖皮质类固醇的有用中间体，该类糖皮质激素在应用场所具有较高的消炎作用，而糖皮质激素的全身作用较低。
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