CAS: 201049-37-8; Epothilone E

上下游产品

Desoxyepothilone E (3S,1E)-1-iodo-2-methylhexa-1,5-dien-3-ol (Z)-(4S,7R,8S,9S,16S)-4,8-Dihydroxy-16-((E)-2-iodo-1-methyl-vinyl)-5,5,7,9-tetramethyl-oxacyclohexadec-13-ene-2,6-dione (3S,6R,7S,8S)-3-(tert-Butyl-dimethyl-silanyloxy)-7-hydroxy-4,4,6,8-tetramethyl-5-oxo-tridec-12-enoic acid (S)-1-((E)-2-iodo-1-methyl-vinyl)-but-3-enyl ester

📜(3S,6R,7S,8S)-3-(Tert-Butyl-Dimethyl-Silanyloxy)-7-Hydroxy-4,4,6,8-Tetramethyl-5-Oxo-Tridec-12-Enoic Acid (S)-1-((E)-2-Iodo-1-Methyl-Vinyl)-But-3-Enyl Ester置于grubbs Catalyst First Generation,四(三苯基膦)钯,双氧水,Potassium Hydrogencarbonate,氟化氢吡啶体系中,用 四氢呋喃,甲醇,二氯甲烷,水,甲苯,乙腈 用作溶剂,化学反应 63.33H,反应生成埃博霉素e
参考文献:通过基于stille偶联的策略进行埃博霉素e和相关侧链修饰类似物的全合成.
标题:通过基于stille偶联的策略进行埃博霉素e和相关侧链修饰类似物的全合成.
摘要:已利用stille偶联策略完成了从乙烯基碘7和噻唑-锡烷8H合成埃博霉素e的全过程.使用闭环复分解(rcm)由三烯15制备中心核心片段7及其反式异构体11,随后将其与多种替代的锡烷偶联以提供埃坡霉素类似物18A-O和19A-O的文库.然后使用stille偶联方法从关键的大内酯中间体24制备埃博霉素b类似物,该中间体本身是通过基于大内酯化的策略合成的.
Doi:10.1016/s0968-0896(98)00153-9

专利信息

专利号:US-8513429-B2
优先权日:2002-08-23
标 题:Synthesis of epothilones, intermediates thereto and analogues thereof
发明人：DANISHEFSKY SAMUEL J; RIVKIN ALEXEY; FUMIKIKO YOSHIMURA; CHOU TING-CHAO; GABARDA ANA E; DONG HUAJIN
权利人:DANISHEFSKY SAMUEL J; RIVKIN ALEXEY; FUMIKIKO YOSHIMURA; CHOU TING-CHAO; GABARDA ANA E; DONG HUAJIN; SLOAN KETTERING INSITUTE FOR CANCER RES
摘要:The present invention provides compounds of formula (I): n n n n n n n n n n n n as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

专利号:US-2023382819-A1
优先权日:2020-10-14
标 题:Processes for synthesis of alpha-emitting radiopharmaceuticals
发明人：MORSE DAVID L; WADAS THADDEUS J; PANDYA DARPAN; TAFRESHI NARGES; BUDZEVICH MIKALAI
权利人:H LEE MOFFITT CANCER CT & RES; UNIV IOWA RES FOUND
摘要:The present disclosure provides processes for the preparation of alpha emitting radiopharmaceutical compositions, in particular DOTATATE complexes of alpha emitting radionuclides, as well as use of such prepared compositions in the treatment of cancers.

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

专利号:US-7067286-B2
优先权日:1998-11-20
标 题 :Cystobacterineae host cells containing heterologous PKS genes for the synthesis of polykedtides
发明人：JULIEN BRYAN; KATZ LEONARD; KHOSLA CHAITAN
权利人:KOSAN BIOSCIENCES INC
摘要:Recombinant host cells of the suborder Cystobacterineae, genus Stizmatella , containing recombinant expression vectors that encode heterologous epothilone polyketide synthase (PKS) genes and can produce epothilones at high levels are provided.

专利号:CA-2556692-A1
优先权日:2004-02-27
标题 :Synthesis of epothilones, intermediates thereto, analogues and uses thereof

专利号:CA-2496477-C
优先权日:2002-08-23
标 题 :Synthesis of epothilones, intermediates thereto, analogues and uses thereof