CAS: 67526-95-8; (3S,3Ar,4S,6S,6Ar,7S,8S,9Bs)-6-Acetoxy-4-(Butyryloxy)-3,3A-Dihydroxy-3,6,9-Trimethyl-8-(((Z)-2-Methylbut-2-Enoyl)Oxy)-2-Oxo-2,3,3A,4,5,6,6A,7,8,9B-Decahydroazuleno[4,5-B]Furan-7-Yl Octanoate

上下游产品

butanoic acid anhydride 8-DebutanoylthapsigarginO8-Debutanoylthapsigargin

📜(2As,2A1R,5As,7S,7As,9S,10R,10Ar,10Bs)-9-((Tert-Butyldiphenylsilyl)Oxy)-2A1,7-Dihydroxy-2A,4,4,7,10-Pentamethyldecahydro-1,3,5-Trioxabenzo[cd]Cyclopenta[h]Azulen-2(2Ah)-One置于盐酸,4-二甲氨基吡啶,丁硫醇,Zinc Borohydride,四丁基氟化铵,氧气,二甲基二环氧乙烷,碳酸氢钠,Potassium Carbonate,戴斯-马丁氧化剂,对甲苯磺酸,臭氧,三乙胺,二异丙胺,N,N-二异丙基乙胺,Magnesium Bromide,Lithium Hexamethyldisilazane体系中,用 四氢呋喃,甲醇,乙醚,二氯甲烷,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应 215.25H,反应生成 毒胡萝卜素
参考文献:五种毒胡萝卜素的总合成:表现出亚纳摩尔serca抑制作用的愈创木酚内酯天然产物.
标题:五种毒胡萝卜素的总合成:表现出亚纳摩尔serca抑制作用的愈创木酚内酯天然产物.
摘要:在这里,我们描述了五种愈创木酚内酯天然产物的总合成:Thapsigargin,Thapsivillosin C,Thapsivillosin F,Trilobolide和nortrilobolide.毒胡萝卜素的前药衍生物已显示出对前列腺肿瘤的选择性体内细胞毒性,并且对该现象的进一步研究的需要凸显了这些总合成的重要性.还描述了毒胡萝卜素c的第一个绝对立体化学分配.
DOI:10.1002/chem.200700302

专利信息

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

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-11155562-B2
优先权日:2014-06-30
标 题 :Synthesis of halichondrin analogs and uses thereof
发明人：KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE
权利人:HARVARD COLLEGE
摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.

专利号:US-10342858-B2
优先权日:2015-01-24
标题 :Glycan conjugates and methods of use thereof
发明人：WONG CHI-HUEY; WU CHUNG-YI
权利人:ACADEMIA SINICA
摘要:The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series 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 globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. 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.

专利号:US-9422259-B2
优先权日:2011-01-18
标题:Synthetic transtaganolide and basiliolide products, derivatives thereof, and synthesis methods thereof
发明人：NELSON HOSEA; MURAKAMI KEI; VIRGIL SCOTT C; STOLTZ BRIAN M; GORDON JONATHAN R
权利人:CALIFORNIA INST OF TECHN
摘要:Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.