Synthesis method of 7-ketolithocholic acid and ursodesoxycholic acid

• Main Authors: LI CHENCHEN, LIN LIN, YE RUFEI, GU XIANGZHONG, QIU WENWEI
• Format: Patent
• Language: Chinese; English
• Published: 21.03.2023
• Subjects: CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY; STEROIDS

The invention belongs to the technical field of organic chemical synthesis or drug synthesis, and particularly relates to a synthesis method of 7-ketolithocholic acid and ursodesoxycholic acid. The synthesis method comprises the following steps: carrying out 3, 7-carbonyl reduction reaction on 3, 7-diketocholanic acid and a hydrogenation reagent under the catalytic conditions of alkali and raney nickel to obtain ursodesoxycholic acid; or the 3, 7-diketocholic acid and the hydrogenation reagent are subjected to a 3-carbonyl selective reduction reaction under the catalysis of raney nickel to obtain 7-ketolithocholic acid, and then the 7-ketolithocholic acid and the hydrogenation reagent are subjected to a 7-carbonyl reduction reaction under the catalysis of alkali and raney nickel to obtain ursodesoxycholic acid. The synthetic route is simple and convenient to operate, environment-friendly and relatively high in yield. 本发明属于有机化学合成或药物合成技术领域，具体涉及一种7-酮基石胆酸及熊去氧胆酸的合成方法。所述合成方法包括：将3,7-二酮基胆烷酸在碱、雷尼镍催化条件下与氢化试剂发生3、7位羰基还原反