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在螺旋内酯甾的结构与疗效关系研究中,我们准备用17α-羟基-17β-醛基化合物(Ⅰ)为原料以合成具反式构型的螺旋内酯甾(Ⅱ)。Ⅰ系未知体。为证明其结构曾用改良的Kishner-Wolff还原法处理。Ⅰ还原后得一混合物,经氧化铝层析获得化合物(Ⅲ)及(Ⅳ),其纯品得率分别为13％及45％,两者均为已知体。Ⅳ经Oppenauer氧化成17β-甲基异睾丸素(Ⅴ);Ⅲ经微量臭氧氧化生成甲醛,因而得到进一步的证明。α-酮醇在用改良的Kishner-Wolff法还原时,α位置的羟基往往易被除去,而现在含α-羟基的醛基化合物(Ⅰ)经还原则主要生成羟基保留之物(Ⅳ)。我们取与Ⅰ结构极为相似的α-
In the study of the relationship between the structure and therapeutic effect of spironolactone, we prepared 17α-hydroxy-17β-aldehyde compound (Ⅰ) as starting material to synthesize spirolactone (Ⅱ) in trans configuration. Ⅰ Department of unknown body. To demonstrate its structure, a modified Kishner-Wolff reduction method was used. After reduction, a mixture was obtained. The compounds (III) and (IV) obtained by alumina chromatography gave 13% and 45% pure products respectively, both of which were known. Ⅳ was oxidized by Oppenauer to 17β-methylisofsorarin (Ⅴ); Ⅲ was oxidized by trace ozone to form formaldehyde, so further evidence was obtained. The α-ketoalcohol tends to be easily removed at the α position when it is reduced by the improved Kishner-Wolff method. Now, the α-hydroxy aldehyde compound (I) is reduced to mainly form the hydroxy group-retaining compound (IV). We take very similar to Ⅰ structure α-