Cyclopentyl Tosylate 反应生成碘代环戊烷 参考文献:碘化镁与甲苯磺酸盐的反应 标题:碘化镁与甲苯磺酸盐的反应 摘要:Mgi 2与甲苯磺酸酯的反应可得到高产率的烷基碘.取决于原料的结构,机理是s N 1或s N 2;在某些情况下,观测到消除产物. Doi:10.1039/c3973000821B
专利信息
专利号:WO-2017082924-A1 优先权日:2015-11-13 标题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE TERRENCE R JR; HYMEL DAVID 权利人:THE US SECRETARY DEPT OF HEALTH & HUMAN SERVICES 摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
专利号:US-9346851-B2 优先权日:2008-02-22 标 题 :Chemical modification of proteins 发明人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN 权利人:BERNARDES GONCALO; CHALKER JUSTIN; DAVIS BENJAMIN; RP SCHERER TECHNOLOGIES LLC 摘要:The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
专利号:US-4033949-A 优先权日:1976-04-14 标 题:Analogs of thromboxane B2 and processes for their synthesis 发明人:KELLY ROBERT C; NELSON NORMAN A 权利人:UPJOHN CO 摘要:The present specification provides novel intermediates and novel processes for the synthesis of various side chain and skeletal analogs of Thromboxane B 2 (11β-homo-11a-oxa-PGF 2 .sub.α). These analogs are particularly and especially useful as reproductive cycle control agents.
专利号:US-10975096-B2 优先权日:2014-06-20 标题 :Synthesis of polycyclic-carbamoylpyridone compounds 发明人:CHIU ANNA; ENQUIST JR JOHN; GRIGGS NOLAN; HALE CHRISTOPHER; IKEMOTO NORIHIRO; KEATON KATIE ANN; KRAFT MATT; LAZERWITH SCOTT E; LEEMAN MICHEL; PENG ZHIHUI; SCHRIER KATE; TRINIDAD JONATHAN; VAN HERPT JOCHEM; WALTMAN ANDREW W 权利人:GILEAD SCIENCES INC 摘要:Methods of making compounds of Formula I are disclosed:
专利号:US-12221419-B2 优先权日:2022-03-30 标题:Abietanes and methods of making and using the same 发明人:FREDERICH JAMES H; SOLANS MEGAN M 权利人:FLORIDA STATE UNIV RESEARCH FOUNDATION INCORPORATED; UNIV FLORIDA STATE RES FOUND 摘要:In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein is versatile polyene cyclization strategy that exploits conjugated β-ionyl derivatives. Photomediated disruption of the extended Ï€-system within these chromophores unveils a contra-thermodynamic polyene that engages in a Heck-type cyclization to afford [4.4.1]-propellanes. The connectivity of overbred polycycles generated from this process is controlled by the position of the requisite C-Halide bond. Thus, compared to conventional biomimetic polyene cyclization, this approach allows for complete control of regiochemistry and facilitates incorporation of both electron-rich and electron-deficient (hetero)aryl groups. This strategy was successfully applied to the total synthesis of abietanes such as, for example, taxodione and salviasperanol, two isomeric abietane-type diterpenes that previously could not be prepared along the same synthetic pathway.
专利号:US-2023285442-A1 优先权日:2020-03-26 标题 :Use of oligochitosans and derivatives thereof for neutralizing viral agents 发明人:MOHAPATRA SUBHRA; MOHAPATRA SHYAM S; Garay Julio; HANNA MAZEN; MAYILSAMY KARTHICK 权利人:MOHAPATRA SUBHRA; MOHAPATRA SHYAM S; Garay Julio; HANNA MAZEN; MAYILSAMY KARTHICK 摘要:Described herein are methods for neutralizing a virus. The methods involve interacting the virus with an oligochitosan or a derivative thereof having a molecular weight of at least 1 KDa and a degree of deacetylation of at least 1%. The methods described herein have numems applications with respect to the treatment or prevention of viral infections caused by a human immunodeficiency virus, a paramyxovirus, an orthomyxovirus, a coronavirus, or a filovirus as well as the detection and quantification of viral load. Also described herein are the synthesis of the oligochitosan and derivatives thereof.
[参考文献]: Raveendra-Panickar Dhanya, Et Al. Design And Synthesis Of An Orally Active Metabotropic Glutamate Receptor Subtype-2 (Mglur2) Positive Allosteric Modulator (Pam) That Decreases Cocaine Self-Administration In Rats. J Med Chem. 2011 Jan 13;54(1):342-53.
合成参考文献
摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 51. 摘要:Iskra, J., Science of Synthesis Knowledge Updates, (2015) 2, 388. 摘要:Singh, F. V.; Wirth, T., Science of Synthesis Knowledge Updates, (2015) 2, 420. 摘要:Yorimitsu, H.; Oshima, K., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 666. 摘要:Li, L.; Biscoe, M. R., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 817.