CAS: 153415-45-3; Taxol C

上下游产品

CAS号133524-70-6 3'-N-debenzoyltaxol | CAS号142-62-1 正己酸

📜3'-N-Debenzoyl-3'-N-Troc-7-Troc-Paclitaxel置于1-羟基苯并三唑,溶剂黄146,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,锌体系中,用 乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应 11.0H,反应生成紫杉醇 C
参考文献:No Auxiliary,No Byproduct Strategy For Water-Soluble Prodrugs Of Taxoids: Scope And Limitation Of O−n Intramolecular Acyl And Acyloxy Migration Reactions
标题:No Auxiliary,No Byproduct Strategy For Water-Soluble Prodrugs Of Taxoids: Scope And Limitation Of O−n Intramolecular Acyl And Acyloxy Migration Reactions
摘要:Since Numerous New Taxoids Active Against Multidrug Resistant (Mdr) Tumors Have Been Developed And Their Poor Water-Solubility Is A Very Real Problem In Intravenous Administration,We Have Designed And Synthesized A Series Of Novel Water-Soluble Taxoid Prodrugs (Isotaxoids). These Prodrugs,A 2'-O-Isoform Of Taxoids,Showed Promising Results With Higher Water Solubility (0.8-1.1 Mg/ml) And Proper Kinetics For Parent Drug Release By A Simple Ph-Dependent Chemical Mechanism Via O-N Intramolecular Acyl Migration. No Additional Functional Auxiliaries Are Released During The Conversion To Parent Drugs,Which Would Be An Advantage In Toxicology And General Pharmacology,And The Cost For The Evaluations Of Auxiliary Units In These Fields Could Be Saved In Prodrug Development. In Addition,We Demonstrate For The First Time The Successful Application Of The O-N Intramolecular Acyloxy Migration Reaction In The Prodrug Design,With The Exception Of The Tert-Butyloxycarbonyl Group,And That This Reaction Can Be Provided With No Organic Solvent And No Side Products.
Doi:10.1021/jm049344G

专利信息

专利号:US-5488116-A
优先权日:1992-03-30
标 题:Total synthesis of taxol and analogues thereof
发明人：DANISHEFSKY SAMUEL J; BORNMANN WILLIAM G; QUENEAU YVES; MAGEE THOMAS V; KROL WALTER J; MASTERS JOHN J; JUNG DAVID K
权利人:SLOAN KETTERING INST CANCER
摘要:The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.

专利号:US-6348337-B1
优先权日:1998-08-18
标题:Process for the preparation of C-4 deacetyltaxanes
发明人：HANSON RONALD L; PATEL RAMESH N
权利人:BRISTOL MYERS SQUIBB CO
摘要:A process useful for the preparation of intermediates in synthesis or semi-synthesis of paclitaxel analogs wherein a starting taxane such as 10-deacetylbaccatin III is deacetylated at the C-4 position using a microorganism or an enzyme derived therefrom to provide 4-deacetyltaxanes, such as 4,10-dideacetylbaccatin III.

专利号:AU-2007245085-A1
优先权日:2006-03-27
标题:A convergent process for the synthesis of taxane derivatives

专利号:CN-115125222-A
优先权日:2021-03-24
标题 :Catalytic Synthesis of Paclitaxel and Its Analogs Using 10-Deacetylbaccatine III10β-O-Acetyltransferase Mutants

专利号:WO-2011134067-A1
优先权日:2010-04-29
标题 :Novel amino acid molecule and uses thereof
发明人：LIU JIAN
权利人:CANADA INC 6570763; LIU JIAN
摘要:There is provided novel amino acid molecules and processes for their preparation. There is also provided novel amino acid molecules and their use in processes for preparing the compounds that are useful for the synthesis of paclitaxel, and docetaxel, the anticancer drug.

专利号:CN-107418938-B
优先权日:2016-05-24
标 题:10-deacetylbaccatin III 10 beta-O-acetyltransferase mutant and application thereof in catalytic synthesis of paclitaxel and analogues thereof