📜2-戊醇置于n,N-二乙基(2-氯-1,1,2-三氟乙基)胺体系中,用 氯仿 用作溶剂,化学反应 15.0H,以76%的收率获得氟环戊烷 参考文献:Process For Producing Fluoro-Compounds 标题:Process For Producing Fluoro-Compounds 摘要:本发明提供了一种利用成本较低且易于处理的n-(2-氯-1,1,2-三氟乙基)二乙胺生产高纯度氟化合物的方法.该方法几乎不产生氯化副产物.具体而言,本发明提供了一种生产氟化合物的方法,包括将由下述通式(1)表示的醇衍生物进行氟化:R1R2R3Coh (其中r1代表氢原子,取代或未取代的烷基,芳基,烷基羰基,烷氧羰基,芳基羰基或芳氧羰基;R2和r3分别独立地代表取代或未取代的烷基,芳基,烷基羰基,烷氧羰基,芳基羰基或芳氧羰基,其中r1,R2和r3中的至少两个可以共同形成环结构,带有或不带有杂原子)与n,N-二乙基-2-氯-1,1,2-三氟乙基胺反应,形成由下述通式(2)表示的氟化合物:R1R2R3Cf (其中r1,R2和r3如上所定义),其特征在于向反应体系中加入由下述通式(3)表示的醇衍生物:R4Oh (其中r4代表取代或未取代的烷基或芳基).
专利信息
专利号:US-2021107859-A1 优先权日:2018-04-06 标题 :A process for the synthesis of carbon labeled organic compounds 发明人:AUDISIO DAVIDE; CANTAT THIBAULT; DESTRO GIANLUCA 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A process for the synthesis of a carbon labeled organic compound containing a carbon labeled carboxyl group is described. A method of using carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; a process for manufacturing labeled pharmaceuticals and agrochemicals comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; and a process for producing tracers comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure are also described.
专利号:US-10065985-B2 优先权日:2015-02-03 标题 :Method for fully automated synthesis of 16β-18F-fluoro-5α-dihydrotestosterone (18F-FDHT) 发明人:MURPHY JENNIFER MARIE; LAZARI MARK SAUL 权利人:UNIV CALIFORNIA 摘要:The automated synthesis of clinically relevant amounts of 16β- 18 F-fluoro-5α-dihydrotestosterone ( 18 F-FDHT) using a commercially available radiosynthesizer. Synthesis was performed in 90 minutes with a decay-corrected radiochemical yield of 29±5%. The specific activity was 4.6 Ci/μmol (170 GBq/μmol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated 18 F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.
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-8461298-B2 优先权日:2004-11-01 标 题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL 权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:US-9260371-B2 优先权日:2004-11-01 标题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN RUTH; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; SLETTEN ELLEN MAY 权利人:UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:WO-2016071243-A1 优先权日:2014-11-05 标 题:Process for preparing halogenated alkenone ethers and their use in the synthesis of anthranilamide pesticides 发明人:BENSON STEFAN; ZIERKE THOMAS; GOETZ ROLAND; WALK BERNHARD; DOMRES MONIKA 权利人:BASF SE 摘要:The present invention relates to a process for preparing a compound of formula (III) starting from the vinyl ether (IlIa) and the compound (IIIb) with a reagent (lllc) selected from the group of sulfonylhalides or sulfonylanhydrides, e.g. methanesulfonyl chloride or p-toluenesulfonyl chloride, in the presence of a base. The present invention relates also to processes comprising further preceding and/or subsequent reaction steps, leading to anthranilamide pesticides or to precursors for them.