CAS: 189453-10-9; Epothilone D

上下游产品

CAS号189453-35-8 (4S,7R,8S,9S,13... | CAS号350493-61-7 (E)-9,10-dehydr... | CAS号187283-46-1 (3S)-2-methyl-1... | CAS号106921-60-2 2,2-二甲基-3-氧代戊醛 | CAS号184246-38-6 (2E)-2-Methyl-3... | CAS号218614-16-5 (-)-(2Z,5S,6E)-... | CAS号371979-40-7 10,11-didehydro... | CAS号187283-44-9 (5S)-5-(tert-bu... | CAS号152044-54-7 埃博霉素B

(E)-9,10-Dehydro-12,13-Desoxyepothilone B置于trisnhnh2,三乙胺体系中,用 1,2-二氯乙烷 用作溶剂,化学反应 7.0H,以91%的收率获得埃博霉素
参考文献:药物发现过程中的复杂靶向全合成:发现极具前景的第二代埃坡霉素家族
标题:药物发现过程中的复杂靶向全合成:发现极具前景的第二代埃坡霉素家族
摘要:描述了埃坡霉素 D 的 (E)-9,10-脱氢衍生物家族(即 12,13-脱氧埃坡霉素 B)的全合成.该路线特别简洁,适合生产新的同类物.此外,本文描述的化学构成了 Epod 全合成的主要简化,这是在人类临床试验中.相对于 D 系列中的野生型饱和类似物,这个新的埃坡霉素家族在其效力和药物稳定性方面显示出主要优势.从通过合成,效力和药代动力学特性的化合物可用性的角度来看,这些化合物很可能保证推进人类临床评估.
Doi:10.1021/ja029695P

专利信息

专利号:US-2004018598-A1
优先权日:2000-05-30
标题 :Bio-intermediates for use in the chemical synthesis of polyketides
发明人：SANTI DANIEL; ASHLEY GARY; MYLES DAVID C
摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.

专利号:US-6350878-B1
优先权日:1998-05-18
标 题 :Intermediates for the synthesis of epothilones and methods for their preparation
发明人：ALTMANN KARL-HEINZ; BAUER ARMIN; SCHINZER DIETER
权利人:NOVARTIS AG
摘要:The invention relates to a method of synthesis for a compound of formula (I),wherein R is a heterocyclyl moiety and X1, X2, X3 and X4 are, independently of each other, protecting groups, which is appropriate for the synthesis of epothilone B and desoxyepothione B.

专利号:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

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-2005043376-A1
优先权日:1996-12-03
标题:Synthesis of epothilones, intermediates thereto, analogues and uses thereof
发明人：DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A
摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.