CAS: 208518-52-9; (1S,3S,7S,10R,11S,12S,16R)-7,11-Dihydroxy-3-((E)-1-(2-(Hydroxymethyl)Thiazol-4-yl)Prop-1-En-2-yl)-8,8,10,12,16-Pentamethyl-4,17-Dioxabicyclo[14.1.0]Heptadecane-5,9-Dione

上下游产品

2-hydroxymethyl-4-tri-n-butylstannylthiazole epothilone B 21-hydroxy-12,13-desoxyepothilone B (Z)-(4S,7R,8S,9S,16S)-8-Hydroxy-16-[(E)-2-(2-hydroxymethyl-thiazol-4-yl)-1-methyl-vinyl]-5,5,7,9,13-pentamethyl-4-triethylsilanyloxy-oxacyclohexadec-13-ene-2,6-dione

📜埃博霉素b置于2,6-二甲基吡啶,间氯过氧苯甲酸,三氟乙酸酐体系中,用 二氯甲烷 用作溶剂,化学反应 3.34H,反应生成埃博霉素f
参考文献:埃坡霉素 Ac 的 N-氧化和 O-酰基重排为 C-19-和 C-21-取代的埃坡霉素.
标题:埃坡霉素 Ac 的 N-氧化和 O-酰基重排为 C-19-和 C-21-取代的埃坡霉素.
摘要:埃坡霉素全合成的最后一步中的一个麻烦的副反应导致形成噻唑-N-氧化物 1.从发酵制备的埃坡霉素中获得,这些具有生物活性的 N-氧化物可以极短地合成高活性埃坡霉素2 具有通过 O-酰基重排修饰的侧链.
Doi:10.1002/(Sici)1521-3773(19990712)38:13/14<1971::Aid-Anie1971>3.0.Co;2-X

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-6930187-B2
优先权日:2002-02-15
标题:Method of preparation of 21-amino epothilone derivatives
发明人：FAVREAU DENIS; KANT JOYDEEP; LEVESQUE KATHIA; WANG SHAOPENG; GUO ZHENGRONG; JAMES BRIAN LESLIE
权利人:BRISTOL MYERS SQUIBB CO
摘要:An improved method of synthesis of 21-amino epothilone derivatives which provides a one-pot conversion of 21-hydroxy epothilones to highly desirable 21-amino epothilones in high yield.

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-2003176368-A1
优先权日:2001-09-06
标题:Synthesis of epothilones, intermediates thereto and analogues thereof
发明人：DANISHEFSKY SAMUEL J; BISWAS KAUSTAV; CHAPPELL MARK; LIN HONG; NJARDARSON JON T; LEE CHUL BOM; RIVKIN ALEXY; CHOU TING-CHAO
摘要:The present invention provides compounds of formula (I): 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-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-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.