CAS: 30562-34-6; (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-Hydroxy-8,14,19-Trimethoxy-4,10,12,16-Tetramethyl-3,20,22-Trioxo-2-Azabicyclo[16.3.1]Docosa-1(21),4,6,10,18-Pentaen-9-Yl Carbamate

上下游产品

CAS号76045-71-1 3-氨基-5-羟基苯甲酸 | CAS号326606-26-2 (3S,5S,6S)-3-[(... | CAS号467214-20-6 阿螺旋霉素 | CAS号75747-14-7 坦螺旋霉素 | CAS号64202-81-9 17-氨基格尔德霉素

19-Iodogeldanamycin置于tris(Dibenzylideneacetone)Dipalladium(0) Chloroform Complex,Copper(L) Iodide,四甲基锡,三苯基膦体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 16.0H,以80%的收率获得格尔德霉素
参考文献:新型格尔德霉素衍生物的合成
标题:新型格尔德霉素衍生物的合成
摘要:当用作热休克蛋白-90抑制剂分子治疗剂时,与苯并醌安沙霉素的格尔德霉素家族相关的毒性可通过在19位上取代来改善.所得的19-取代的衍生物具有更大的潜力,可用于肿瘤临床试验和其他医学目的,例如神经退行性疾病的治疗.通过各种合成方法克服了与这些分子的敏感性和复杂性相关的障碍,本文报道了使用优化的stille和suzuki偶联反应合成一系列19-取代的格尔德霉素衍生物.其他化合物可通过以下途径获得 铜介导的偶联和亲核加成反应由于与先前在临床上评估的19种未取代对应物相比,以前针对此类底物观测到的毒性显着降低,因此这些新化合物具有重要的医学意义.
Doi:10.1016/j.Tet.2021.131927

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-2024197774-A1
优先权日:2021-04-16
标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
发明人：LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
权利人:UNIV TEXAS
摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

专利号:US-2025090698-A1
优先权日:2018-11-27
标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases
发明人：CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT
权利人:INDIAN INSTITUTE OF TECH INDORE
摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.

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-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.