专利号:US-4592874-A 优先权日:1980-05-14 标 题:Process for the synthesis of alpha-chlorinated chloroformates 发明人:CAGNON GUY C; PITEAU MARC D; SENET JEAN-PIERRE G; OLOFSON ROY A; MARTZ JONATHAN T 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:Process for the synthesis of alpha -chlorinated chloroformates, and new alpha -chlorinated chloroformates. The invention relates to a new process for the manufacture of alpha -chlorinated chloroformates and, to new alpha -chlorinated chloroformates as new industrial products. The process according to the invention consists of a synthesis, by catalytic phosgenation, of alpha -chlorinated chloroformates of the formula: in which: R represents a substituted or unsubstituted hydrocarbon radical and m represents an integer superior or equal to one, this synthesis consisting in reacting phosgene with the aldehyde R-CHO)m, in the presence of a catalyst which is an organic or inorganic substance which is capable in a medium containing an aldehyde of the formula R-CHO)m, phosgene and, possibly, a solvent, of generating a pair of ions one of which is an halogenide anion and the other is a cation which is sufficiently separated from said halogenide anion so as to give to the latter a nucleophilic power enabling it to react with the function(s) aldehyde of the molecule R-CHO)m.
专利号:US-9085518-B2 优先权日:2011-10-14 标题 :Method for the synthesis of 18F-labelled molecules 发明人:NAIRNE ROBERT JAMES DOMETT; BHALLA RAJIV; KHAN IMTIAZ; BROWN JANE; WILSON ANTHONY; BLACK ANDRES 权利人:GE HEALTHCARE LTD 摘要:The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, in a preferred embodiment, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimized.
专利号:US-2015239796-A1 优先权日:2014-02-19 标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane 发明人:RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS 权利人:UNIV OSLO 摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).
专利号:US-11851407-B2 优先权日:2016-06-10 标 题 :Synthesis of the radiolabeled prostate-specific membrane antigen (PSMA) inhibitor [18F]DCFPYL 发明人:RAVERT HAYDEN T; HOLT DANIEL P; CHEN YING; MEASE RONNIE C; FAN HONG; POMPER MARTIN G; DANNALS ROBERT F 权利人:UNIV JOHNS HOPKINS; THE JOHNS HOPKINS UNIVERSTY 摘要:Methods, and related compositions, for the improved synthesis of [ 18 F]DCFPyL are disclosed. Also provided are methods, and related compositions, for the use of [ 18 F]DCFPyL so produced.
专利号:US-9125954-B2 优先权日:2011-10-14 标 题 :Method for the synthesis of 18F-labelled biomolecules 发明人:BHALLA RAJIV; WILSON ANTHONY; KHAN IMTIAZ; BROWN JANNE 权利人:GE HEALTHCARE LTD 摘要:The present invention provides a method for the synthesis of 18 F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimized.
专利号:US-2016222024-A1 优先权日:2013-09-20 标 题:S-enantiomer of tetracyclic indole derivative as pbr ligands 发明人:TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER 权利人:GE HEALTHCARE LTD 摘要:The present invention concerns in vivo imaging and in particular in vivo imaging of translocator protein (TSPO, formerly known as the peripheral benzodiazepine receptor). An indole-based in vivo imaging agent is provided that overcomes problems relating to known TSPO-binding radiotracers. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said precursor compound. Other aspects of the invention include a method for the synthesis of the in vivo imaging agent of the invention comprising use of the precursor compound of the invention, a kit for carrying out said method, and a cassette for carrying out an automated version of said method. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
参考文献:10.1107/s1600536811018873 摘要:Ellis TK, Clayton SM, Powell DR, Taylor RW. 21-(4-Methyl-phenyl-sulfon-yl)-4,7,13,16-tetra-oxa-1,10,21-triaza-bicyclo-[8.8.5]tricosane-19,23-dione: an N-tosyl-ated macrobicyclic dilactam. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1533. 参考文献:10.1007/s00259-011-1879-9 摘要:Miao Z, Ren G, Jiang L, Liu H, Webster JM, Zhang R, Namavari M, Gambhir SS, Syud F, Cheng Z. A novel 18F-labeled two-helix scaffold protein for PET imaging of HER2-positive tumor. European Journal of Nuclear Medicine and Molecular Imaging. 2011 Jul 15;38(11):1977. doi: 10.1007/s00259-011-1879-9. 参考文献:10.1007/128_2011_199 摘要:Mahon E, Aastrup T, Barboiu M. Dynamic nanoplatforms in biosensor and membrane constitutional systems. Top Curr Chem. 2012;322():139–63. doi: 10.1007/128_2011_199.