专利号:US-11161827-B2 优先权日:2019-04-05 标 题 :Catalytic systems for stereoselective synthesis of chiral amines by enantiodivergent radical C—H amination 发明人:Zhang xiao-xiang; Lang kai 权利人:TRUSTEES BOSTON COLLEGE; THE TRUSTEES OF BOSTON COLLEGE 摘要:In one aspect, the disclosure relates to a mode of asymmetric induction in radical processes based on sequential combination of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution. Also disclosed is an asymmetric system for stereoselective synthesis of strained 5-membered cyclic sulfamides via radical 1,5-C—H amination of sulfamoyl azides. The disclosed metalloradical system can control the degree and sense of asymmetric induction in the catalytic radical C—H amination in a systematic manner. The disclosed system is applicable to a broad scope of substrates with different types of C(sp 3 )—H bonds and exhibits reactivity and selectivity, providing access to both enantiomers of useful 5-membered cyclic sulfamides in a highly enantioenriched form. Also disclosed are catalysts useful in these processes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
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-9512096-B2 优先权日:2011-12-22 标题 :Synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds 发明人:CHEN WEIRONG; HUMORA MICHAEL; KWOK DAW-LONG ALBERT; KIESMAN WILLIAM F; IRDAM ERWIN AYANDRA 权利人:KNOPP BIOSCIENCES LLC; KNOPP BIOSCIENCES LLP 摘要:The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.
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-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-8519148-B2 优先权日:2007-03-14 标题 :Synthesis of chirally purified substituted benzothiazole diamines 发明人:RAJE PRASAD; GADIKOTA RAJENDRAKUMAR REDDY; CHEN JIAN-XIE; LAPINA OLGA V; MCCALL JOHN M 权利人:RAJE PRASAD; GADIKOTA RAJENDRAKUMAR REDDY; CHEN JIAN-XIE; LAPINA OLGA V; MCCALL JOHN M; KNOPP NEUROSCIENCES INC 摘要:Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003). 摘要:Shcherbakova, I., Science of Synthesis, (2007) 31, 800. 摘要:Lawrence, S. A., Science of Synthesis, (2009) 40, 511.