CAS: 80663-95-2; 1-(3-Iodobenzyl)Guanidine

上下游产品

3-iodobenzylamine tetrabutylammonium thi°Cyanate 2-methylisothiourea sulphate m-iodobenzylguanidine dihydrogen carbonate131I]-meta-iodobenzylguanidine[131I]-meta-iodobenzylguanidine N-(3-iodobenzyl)-N'-(3-carbonyl-quinoline)guanidine

📜N',N''-Bis(Tert-Butoxycarbonyl)-N-(3-Iodobenzyl)Guanidine置于盐酸,甲酸体系中,用 水 作为反应溶剂,以93%的收率获得产物间碘苄胍半硫酸
参考文献:用于心脏 Pet 成像的 [11C] 胍的全自动放射合成
标题:用于心脏 Pet 成像的 [11C] 胍的全自动放射合成
摘要:放射性标记的胍如间碘苄基胍(Mibg) 在核医学中用作诊断显像剂和放射治疗剂,多年来,已经开发了许多将放射性核素掺入胍中的方法.在开发用于心脏交感神经密度的新型正电子发射断层扫描 (Pet) 放射性示踪剂的项目中,我们有理由准备 [11]C]3F-Phpog.然而,很快就发现用碳 11 对胍支架进行放射性标记仍然具有挑战性,而且历史方法缺乏与现代自动放射化学合成平台和当前非常好生产规范 (Cgmp) 要求的兼容性.为了应对这一挑战,我们报告了一种用碳 11 对胍进行放射性标记的新自动化方法.该方法用于制备一系列具有非常好放射化学产率(放射性 HPLC 为 8-76%)的 [11 C] 胍,并发现其具有广泛的底物范围和对未保护的 Oh 和 Nh 官能团的耐受性.该方法用于合成[11C]3F-Phpog 用于临床前成像,以及放射性示踪剂临床前使用的适用性通过新西兰白兔的初步心脏 Pet 得到证明,该
DOI:10.1021/acsmedchemlett.0C00479

专利信息

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-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-6420556-B1
优先权日:1998-12-17
标 题 :Acyl isothiocyanate resins and their use in solid-supported synthesis of guanidines
发明人：WILSON LAWRENCE JOSEPH
权利人:PROCTER & GAMBLE
摘要:The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetranikylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.