2,4,6-三氯苯酚置于potassium Carbonate体系中,用 丙酮 作为反应溶剂,化学反应生成 2,4,6-三氯苯甲酸 参考文献:Bisagni,E.; Rivalle,C.,Bulletin De La Societe Chimique De France,1969,P. 3111-3115 标题:Bisagni,E.; Rivalle,C.,Bulletin De La Societe Chimique De France,1969,P. 3111-3115
专利号:US-7202256-B2 优先权日:2004-04-14 标题:Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779 发明人:GU JIANXIN; RUPPEN MARK E; RAVEENDRANATH PANOLIL; CHEW WARREN; SHAW CHIA-CHENG 权利人:WYETH CORP 摘要:Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
专利号:US-8258299-B2 优先权日:2009-03-27 标题:Process for preparation of temsirolimus 发明人:LEE KWANG-CHUNG; LEE TING-HUEI; TUNG YEN-SHIH; KAO CHIA-CHEN; LEE TZU-AI 权利人:LEE KWANG-CHUNG; LEE TING-HUEI; TUNG YEN-SHIH; KAO CHIA-CHEN; LEE TZU-AI; CHUNGWA CHEMICAL SYNTHESIS & BIOTECH CO LTD 摘要:The present invention provides two synthetic routes for the preparation of Temsirolimus (compound 1b and analog of Temsirolimus 1a). The first route includes the synthesis of CCI-779 by directly reacting rapamycin (4b) or Prolyl-rapamycin (4a) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base, followed by deprotection to give CCI-779 or Proline CCI-779. The second route includes a process involving a reaction of rapamycin-OH-31-sily ether (4d) or Prolyl-rapamycin-OH-31-sily ether (4c) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base and followed by subsequent hydrolysis step to obtain the desired CCI-779 or Proline CCI-779. n Compound 11, as described in this invention, is stable at room temperature, cost effective and ease of processing.
专利号:US-7153957-B2 优先权日:2003-08-07 标 题:Regioselective synthesis of CCI-779 发明人:CHEW WARREN; SHAW CHIA-CHENG 权利人:WYETH CORP 摘要:A method for regioselective synthesis of CCl-779 based on boronate chemistry is provided. Also provided are novel intermediates useful in this method.
专利号:US-9676698-B2 优先权日:2010-07-20 标 题:Method of producing ingenol-3-angelate 发明人:HOGBERG THOMAS; GRUE-SORENSEN GUNNAR; LIANG XIFU; HORNEMAN ANNE MARIE; PETERSEN ANDERS KLARSKOV 权利人:LEO LABORATORIES LTD 摘要:The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). n n n n n n n n n n Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.
专利号:US-2002058286-A1 优先权日:1999-02-24 标 题 :Synthesis of epothilones, intermediates thereto and analogues thereof 发明人:DANISHEFSKY SAMUEL J; STACHEL SHAWN J; LEE CHUL BOM; CHAPPELL MARK D; CHOU TING-CHAO; WU ZHICAI 摘要:The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
专利号:US-6867305-B2 优先权日:1996-12-03 标题:Synthesis of epothilones, intermediates thereto and analogues thereof 发明人:DANISHEFSKY SAMUEL J; STACHEL SHAWN J; LEE CHUL BOM; CHAPPELL MARK D; WU ZHICAL 权利人:SLOAN KETTERING INST CANCER; UNIV COLUMBIA 摘要:The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
[参考文献]: Emeline L Maillet, Et Al. Phenoxy Herbicides And Fibrates Potently Inhibit The Human Chemosensory Receptor Subunit T1R3. J Med Chem. 2009 Nov 12;52(21):6931-5. [参考文献]: Hong-Se Oh, Et Al. Total Synthesis Of Methymycin. Org Biomol Chem. 2009 Nov 7;7(21):4458-63. [参考文献]: Isaac Ayodele Ololade, Et Al. Influence Of Organic Carbon And Metal Oxide Phases On Sorption Of 2,4,6-Trichlorobenzoic Acid Under Oxic And Anoxic Conditions. Environ Monit Assess. 2015 Jan;187(1):4170. [参考文献]: S Moller, Et Al. Impact Of Nutrient Composition On A Degradative Biofilm Community. Appl Environ Microbiol. 1997 Jun;63(6):2432-8.
合成参考文献
参考文献:10.1007/s00244-002-1174-7 摘要:Kukkonen JVK. Lethal Body Residue of Chlorophenols and Mixtures of Chlorophenols in Benthic Organisms. Archives of Environmental Contamination and Toxicology. 2001 Oct 17;43(2):214–20. doi: 10.1007/s00244-002-1174-7.