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ANALOGIFREMGANGMAATE VED FREMSTILLING AV TERAPEUTISK AKTIVE PREGNAN-21-SYREDERIVATER

机译:制备具有治疗活性的PREGNAN-21酸衍生物的类似方法

摘要

Title derivs of formula (I): (where -A-B- is -CH2-CH2-, -CH=CH- or -CCl=CH-; X is H, halogen or CH3; = Y-Z- is =CH-CH2-, =C=CH-, =CV-CHOH-, =CV-CO- or CW-CHW' in which V is a H or halogen and W and W' are halogen; R1 is alkyl and R2 is alkyl or aryl, or R1+R2 is tetra- or pentamethylene; and R3 is H, an alkali metal atom, or an opt. substd. hydrocarbon radical) have excellent local anti-inflammatory action but are practically inactive when administered systemically and are therefore useful for the local treatment of various inflammatory skin disorders. Pref. (I) is prepd by oxidising (I; where OR3 is replaced by H) or their hydrates or hemiacetals with oxidising metal oxides in the presence of alcohol alcohols.
机译:式(I)的标题衍生物:(其中-AB-为-CH 2 -CH 2-,-CH = CH-或-CCl = CH-; X为H,卤素或CH 3; = Y Z-为= CH-CH 2-, = C = CH-,= CV-CHOH-,= CV-CO-或CW-CHW',其中V为H或卤素,W和W'为卤素; R1为烷基,R2为烷基或芳基,或R1 + R2为四亚甲基或五亚甲基; R3为H,碱金属原子或最优取代的烃基)具有出色的局部消炎作用,但在全身给药时几乎没有活性,因此可用于局部治疗各种炎症性皮肤病。首选(I)通过在醇-醇存在下用氧化性金属氧化物氧化(I;其中OR 3被H代替)或它们的水合物或半缩醛制备。

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