CAS: 78755-81-4; Ethyl 8-Fluoro-5-Methyl-6-Oxo-5,6-Dihydro-4H-Benzo[f]Imidazo[1,5-A][1,4]Diazepine-3-Carboxylate

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CAS号428507-28-2 (E)-(dimethylam... | CAS号193693-31-1 2-chloro-7-fluo... | CAS号999-97-3 六甲基二硅氮烷 | CAS号99-97-8 N,N-二甲基对甲苯胺 | CAS号3400-09-7 二氯胺 | CAS号2999-46-4 异氰基乙酸乙酯 | CAS号865-47-4 叔丁醇钾 | CAS号78755-80-3 7-氟-3.4-二氢-4-甲基... | CAS号658075-93-5 8-amino-5,6-dih... | CAS号133368-73-7 3'-fluoropropyl... | CAS号84378-44-9 Ro15-3890游离态

5-甲基-8-硝基-6-氧代-5,6-二氢-4H-苯并[f]咪唑并[1,5-A][1,4]二氮杂卓-3-羧酸乙酯置于palladium On Activated Charcoal 亚硝酸特丁酯,三氟化硼乙醚,氢气体系中,用 四氢呋喃,乙醇,二氯甲烷 作为反应溶剂,化学反应 2.67H,反应生成 氟马西尼
参考文献:一种适用于 Fluorine-18 标记的氟腙新合成方法
标题:一种适用于 Fluorine-18 标记的氟腙新合成方法
摘要:近年来,由于多种因素的共同作用,氟化有机化合物在生物医学领域越来越重要,例如 (I) 碳-氟键的稳定性,特别是在热和氧化降解方面 (II)氟和氢原子的类似空间要求允许类似的代谢途径和(iii)增强的亲脂性,与相应的氢化类似物相比,导致氟化化合物扩散到动物组织中.此外,"*f 标记的底物在正电子发射断层扫描 (Pet) 中充当示踪剂,这构成了体内药代动力学研究和非侵入性临床诊断的有用工具.*然而,由于半衰期(110 分钟)) 的氟 18 核素,只要在合成序列的最后一步掺入氟原子,就可以实现和操纵 18F 标记的底物.不幸的是,在大多数有机氟衍生物的合成中情况并非如此.在与药理学家合作计划的背景下,我们希望获得抗抑郁药氟马西尼 73 及其三唑类似物 10 的新条目,适用于最终的氟
DOI:10.1080/00304940309355361

专利信息

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-2012189547-A1
优先权日:2009-10-08
标 题 :[18f] labelled analogues of flumazenil as in vivo imaging agents
发明人：WOODCRAFT JOHN; JONES CLARE L; GAETA ALESSANDRA; TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER; PLANT STUART
权利人:WOODCRAFT JOHN; JONES CLARE L; GAETA ALESSANDRA; TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER; PLANT STUART
摘要:The present invention provides radiofluorinated compounds useful for in vivo imaging GABA A receptors. Also provided by the present invention is a method of synthesis for the radiofluorinated compounds of the invention, in particular an automated method of synthesis. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention.

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-2005232861-A1
优先权日:2004-04-20
标 题 :Microfluidic apparatus and method for synthesis of molecular imaging probes including FDG
发明人：BUCHANAN CHARLES R; PADGETT HENRY C; COLLIER THOMAS L
权利人:BUCHANAN CHARLES R; PADGETT HENRY C; COLLIER THOMAS L
摘要:The invention provides a method and apparatus for preparation of radiochemicals wherein the reaction that couples the radioactive isotope to the reactive precursor to form a positron-emitting molecular imaging probe is performed in a microfluidic environment. The method comprises: providing a micro reactor; introducing a liquid reactive precursor dissolved in a polar aprotic solvent into an inlet port of the micro reactor, the reactive precursor adapted for reaction with a radioactive isotope to form a radiochemical; introducing a solution comprising a radioactive isotope dissolved in a polar aprotic solvent into another inlet port of the micro reactor; contacting the reactive precursor with the isotope-containing solution in a microchannel of the micro reactor; reacting the reactive precursor with the isotope-containing solution as the reactive precursor and isotope-containing solution flow through the microchannel of the micro reactor, wherein the reacting step is conducted at a temperature above the boiling point of the polar aprotic solvent at 1 atm and at a pressure sufficient to maintain the polar aprotic solvent in liquid form; and collecting the resulting radiochemical from the micro reactor.

专利号:WO-9964032-A1
优先权日:1998-06-08
标题 :Combinatorial synthesis of multibinding libraries
发明人：CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.

专利号:US-8895727-B2
优先权日:2011-05-25
标题 :Method for preparation of fluorine-18-labeled flumazenil using diaryliodonium salt precursor
发明人：LEE BYUNG CHUL; MOON BYUNG SEOK; KIM JI SUN
权利人:BIO IMAGING KOREA CO LTD
摘要:Disclosed is the synthesis of [ 18 F]flumazenil that is useful in imaging epileptic lesions by PET (positron emission tomography). A method for preparing [ 18 F]flumazenil by reacting a diaryliodonium salt precursor with the positron-emitting radionuclide fluorine-18. [ 18 F]flumazenil can be prepared from the diaryliodonium salt precursor in the presence of kryptofix 2.2.2. /potassium carbonate(K 2.2.2. /K 2 CO 3 ) and TEMPO in dimethylformamide (DMF) at a high yield.