Iida T, Momose T, Tamura T, Matsumoto T, Chang F C, Goto J, Nambara T
College of Engineering, Nihon University, Fukushima-ken, Japan.
J Lipid Res. 1988 Feb;29(2):165-71.
New synthetic routes to three possible stereoisomers of hyodeoxycholic (3 alpha, 6 alpha-dihydroxy-5 beta-cholanic) acid are described. The principal reactions involved were inversion at C-3 of 3 alpha-hydroxy-6-oxo derivatives with diethyl azodicarboxylate-triphenylphosphine-formic acid and with N,N-dimethylformamide, without allomerization to the more stable 5 alpha form. On the basis of physical and chromatographic data, previously reported 3 beta, 6 alpha-dihydroxy-5 beta-cholanic acid and its methyl ester are shown to be C-3 epimeric mixtures. The 13C nuclear magnetic resonance spectra were of key importance in characterizing the stereoisomers and estimating their purity.
本文描述了猪去氧胆酸(3α,6α-二羟基-5β-胆烷酸)三种可能的立体异构体的新合成路线。主要反应包括用偶氮二羧酸二乙酯-三苯基膦-甲酸和N,N-二甲基甲酰胺使3α-羟基-6-氧代衍生物在C-3处发生构型翻转,而不会异构化为更稳定的5α形式。根据物理和色谱数据,先前报道的3β,6α-二羟基-5β-胆烷酸及其甲酯被证明是C-3差向异构体混合物。13C核磁共振光谱对于表征立体异构体和评估其纯度至关重要。