N-<(2S,3S)-3-Azido-2-Hydroxy-4-Phenylbutanoyl>-L-Leucine Benzyl Ester置于palladium On Activated Charcoal 氢气体系中,化学反应生成 乌苯美司 参考文献:Synthesis Of Bestatin,A Potent Inhibitor Of Leukotriene A4 Hydrolase,By An N3Nucleophile Reaction To A Non-Protected Diol 标题:Synthesis Of Bestatin,A Potent Inhibitor Of Leukotriene A4 Hydrolase,By An N3Nucleophile Reaction To A Non-Protected Diol 摘要:报道了基于区域选择性引入氮功能基到无保护二醇9上,合成bestatin(1)的方法. DOI:10.1271/bbb.60.534
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-5962515-A 优先权日:1997-05-29 标题 :Process for isolation and synthesis of 1-(3,4 methylenedioxy-phenyl)-1E-tetradecene and its analogues and their activities against tumors and infections 发明人:UPADHYAY SHAKTI N; VISHWAKARMA RAM A; GHOSAL SABARI; SHUKLA SUPRIYA; BOSE CHANDA; KAMRA ANITA 权利人:NAT INST IMMUNOLOGY 摘要:Process for isolation of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene from Piper longum. Processes for synthesis of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene; its stereoisomers and analogues are disclosed. The compounds isolated and synthesized according to this invention have immunomodulatory properties and can be used to treat tumors and infections.
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.
1: Shi Y, Guo Q, Jing F, Shang X, Zhou C, Jing F. Ubenimex suppresses glycolysis mediated by CD13/Hedgehog signaling to enhance the effect of cisplatin in liver cancer. Transl Cancer Res. 2023 Oct 31;12(10):2823-2836. doi: 10.21037/tcr-23-435. Epub 2023 Sep 28. 2: Zhou Z, Huayu M, Mu Y, Tang F, Ge RL. Ubenimex combined with Albendazole for the treatment of Echinococcus multilocularis-induced alveolar echinococcosis in mice. Front Vet Sci. 2024 Mar 15;11:1320308. doi: 10.3389/fvets.2024.1320308. 3: Ota K. Review of ubenimex (Bestatin): clinical research. Biomed Pharmacother. 1991;45(2-3):55-60. doi: 10.1016/0753-3322(91)90123-b.
合成参考文献
参考文献:10.7164/antibiotics.29.100 摘要:Suda H, Takita T, Aoyagi T, Umezawa H. The structure of bestatin. J Antibiot (Tokyo). 1976 Jan;29(1):100–1. doi: 10.7164/antibiotics.29.100.