The Synthesis of the Oxidation of Chenodeoxycholic Acid
作者: 蔡烈峰 ：杭州和泽医药科技有限公司;
Abstract: Objective: Regioselective oxidation of chenodeoxycholic acid in different positions. Methods: The third was oxidized with silver carbonate; the seventh was oxidized with N-bromosuccinimide; the third and the seventh were oxidized with Jones reagent. Results: The synethesis of regioselective oxidation of chenodeoxycholic acid has advantages such as lower cost, higher yield, easier in aftertreatment and more suitable for industrialized production. Conclusion: This synthetic process has advantages such as mild conditions, easy operation, low cost and high yield, and is suitable for large-scale production.
文章引用: 蔡烈峰 (2015) 鹅去氧胆酸的氧化产物合成。 药物化学， 3， 11-14. doi: 10.12677/HJMCe.2015.32002
 郑兴 (2008) 鹅去氧胆酸和熊去氧胆酸的对比研究. 内蒙古科技与经济, 2, 28-32.
 Poša, M. and Kuhajda, K. (2010) Hydrophobicity and haemolytic potential of oxo derivatives of cholic, deoxycholic and chenodeoxycholic acids. Steroids, 75, 424-431.
 Bianchini, E., Chinaglia, N., Dean, M., Giovannini, P.P., Medici, A., Pedrini, P. and Poli, S. (1999) Regiospecific oxi- doreductions catalyzed by a new pseudomonas paucimobilis hydroxysteroid dehydrogenase. Tetrahedron, 55, 1391- 1398.
 Okumura, K., Nakamura, Y., Takeuchi, S., Kato, I., Fujimoto, Y. and Ikekawa, N. (2003) Formal synthesis of squala- mine from desmosterol. Chemical and Pharmaceutical Bulletin, 51, 1177-1182.
 杨先金, 张晓奇 (2013) 一种熊去氧胆酸的制备方法. 中国专利: 103319560.
 黄燕敏, 崔建国, 姚秋翠, 甘春芳, 林启福 (2013) 3-氧代-7-肟基-4-氮杂-A-homo-鹅脱氧胆酸甲酯和3-O-苄肟基-7-氮杂-7α-氧代-β-homo-鹅脱氧胆酸甲酯及其在制备抗肿瘤药物中的应用. 中国专利: 103044518.
 Iguchi, Y., Nishimaki-Mogami, T., Yamaguchi, M., Teraoka, F., Kaneko, T. and Une, M. (2011) Effects of chemical modification of ursodeoxycholic acid on TGR5 activation. Biological & Pharmaceutical Bulletin, 34, 1-7.
 Yu, D., Mattern, D.L. and Forman, B.M. (2012) An improved synthesis of 6a-ethylchenodeoxycholic acid (6ECDCA), a potent and selective agonist for the Farnesoid X Receptor (FXR). Steroids, 77, 1335-1338.
 Fantin, G., Ferrarini, S., Medici, A., Pedrini, P. and Poli, S. (1998) Regioselective microbial oxidation of bile acids. Tetrahedron, 54, 1937-1942.