合成目标产物 Cholic Acid Methyl Ester 主要起始原料 Methanol And Cholic Acid
(文献来源)合成步骤主要原料 Methanol 和 Cholic Acid
胆酸置于盐酸体系中,用 甲醇 用作溶剂,化学反应 12.0H,反应生成胆酸甲酯 参考文献:Novel Liver-Specific Nitric Oxide (No) Releasing Drugs With Bile Acid As Both No Carrier And Targeting Ligand 标题:Novel Liver-Specific Nitric Oxide (No) Releasing Drugs With Bile Acid As Both No Carrier And Targeting Ligand 摘要:Novel Liver-Specific Nitric Oxide (No) Releasing Drugs With Bile Acid As Both The No Carrier And Targeting Ligand Were Designed And Synthesized By Direct Nitration Of The Hydroxyl Group In Bile Acids Or The 3-O-Hydroxyl Alkyl Derivatives,With The Intact 24-Cooh Being Preserved For Hepatocyte Specific Recognition. Preliminary Biological Evaluation Revealed That Oral Administrated Targeted Conjugates Could Protect Mice Against Acute Liver Damage Induced By Acetaminophen Or Carbon Tetrachloride. The Nitrate Level In The Liver Significantly Increased After Oral Administration Of 1E While Nitrate Level In The Blood Did Not Significantly Change. Co-Administration Of Ursodeoxycholic Acid (Udca) Significantly Antagonized The Increase Of Nitrate In The Liver Resulted By Administration Of 1E. (C) 2014 Hui-Fen Wang And Bo-Hua Zhong. Published By Elsevier B.V. On Behalf Of Chinese Chemical Society. All Rights Reserved. Doi:10.1016/j.Cclet.2014.04.001
专利信息
专利号:WO-2023148764-A1 优先权日:2022-02-01 标 题 :Novel cholic acid derivatives for the treatment and prevention of autoimmune diseases and uses thereof 发明人:AWASTHI AMIT; SALUNKE DEEPAK; DALAL RAJDEEP; MADAN UPASNA; SADHU SRIKANT; SINGLA POONAM; KAMBOJ AARZOO; ASTHANA SHAILENDRA 权利人:TRANSLATIONAL HEALTH SCIENCE AND TECH INSTITUTE; PANJAB UNIV 摘要:The present invention is to design and develop novel synthetic cholic acid derivatives for treating autoimmune disorders/inflammatory conditions, process of synthesis of the compounds, compositions comprising the said compounds and use of the compounds and treatment comprising the compounds of the present invention.
专利号:US-10544441-B2 优先权日:2014-06-24 标 题 :Method for biocatalytic whole cell reduction of dehydrocholic acid compounds, and 7-β-hydroxysteroid dehydrogenase mutants 发明人:WEUSTER-BOTZ DIRK; SUN BOQIAO; QUIRIN CHRISTIAN 权利人:PHARMAZELL GMBH 摘要:The invention relates to novel biocatalytic processes comprising the whole cell reduction of dehydrocholic acid (DHCA) compounds, novel 7β-hydroxy steroid dehydrogenase mutants, the sequences coding for these enzyme mutants, methods for producing the enzyme mutants and use thereof in enzymatic conversions of cholic acid compounds, and in particular in the production of ursodesoxycholic acid (UDCA); also a subject of the invention are novel methods for the synthesis of UDCA using the enzyme mutants; and in particular a further improved method for producing UDCA using recombinant whole cell biocatalysts.
专利号:US-4895679-A 优先权日:1989-02-17 标 题 :Process for production of chenodeoxycholic acid and novel intermediates useful for the process 发明人:YOO SEO H 权利人:PRIME CHEMICALS TECHNOLOGY COR 摘要:Novel intermediates useful in the synthesis of chenodeoxycholic acid, the intermediates being of the formula: ##STR1## wherein --X is an electron withdrawing group, n is an integer equal to zero or one, and --Y is a halogen. n A process for producing such novel intermediates from 5β-cholanic acid-3α, 7α, 12α-triol methyl ester is carried out without using highly toxic and carcinogenic compounds such as dichromates and chromium trioxide.
专利号:US-11306343-B2 优先权日:2014-08-12 标 题:3α-hydroxysteroid dehydrogenase mutants and process for the preparation of ursodeoxycholic acid 发明人:HUMMEL WERNER; BAKONYI DANIEL 权利人:PHARMAZELL GMBH 摘要:The invention provides novel 3α-hydroxysteroid dehydrogenase mutants, sequences that code for these enzyme mutants, methods for producing the enzyme mutants, and the use thereof in enzymatic reactions of cholic acid compounds, and in particular in the production of ursodeoxycholic acid (UDCA). The invention further provides processes for the synthesis of UDCA using the enzyme mutants and the production of UDCA using recombinant microorganisms that have been subjected to multiple modifications.
专利号:US-5627270-A 优先权日:1991-12-13 标题:Glycosylated steroid derivatives for transport across biological membranes and process for making and using same 发明人:KAHNE DANIEL E; KAHNE SUZANNE W; SOFIA MICHAEL J; HATZENBUHLER NICOLE T 权利人:UNIV PRINCETON; TRANSCELL TECHNOLOGIES INC 摘要:Novel glycosylated steroid derivatives for facilitating the transport of compounds across biological membranes, either in admixture or as conjugates, are disclosed. A novel process for efficient synthesis of these glycosylated steroid derivatives, using activated glycosyl sulfoxide intermediates is provided. Methods for the permeabilization of membranes and the enhancement of the activity of predetermined compounds are also provided.
专利号:EP-2327790-A1 优先权日:2009-11-30 标 题:New 7ß-hydroxy steroid dehydrogenases and their use 权利人:PHARMAZELL GMBH 摘要:The invention relates to novel 7β-hydroxysteroid dehydrogenases obtainable from bacteria of the genus Collinsella, in particular of the strain Collinsella aerofaciens, the sequences coding for these enzymes, processes for the preparation of the enzymes and their use in enzymatic reactions of cholic acid compounds, and in particular in the preparation of ursodeoxycholic acid ( UDC); The invention also provides novel methods for the synthesis of UDCS.
参考文献:10.5281/zenodo.5794106 摘要:The LOTUS Initiative for Open Natural Products Research: frozen dataset union wikidata (with metadata) | DOI:10.5281/zenodo.5794106 参考文献:10.1007/bf03190713 摘要:Kuhajda K, Kevresan S, Kandrac J, Fawcett JP, Mikov M. Chemical and metabolic transformations of selected bile acids. European Journal of Drug Metabolism and Pharmacokinetics. 2006 Sep;31(3):179–235. doi: 10.1007/bf03190713.