专利号:US-9988364-B1 优先权日:2017-03-21 标题 :Process for synthesis of Eliglustat and intermediate compounds thereof 发明人:LIU YU; YU GUANNENG; ZHENG ZHIGUO 权利人:ZHEJIANG AUSUN PHARMACEUTICAL CO LTD 摘要:The present invention relates to a process for synthesis of Eliglustat and intermediate compounds thereof. In particular, the present invention relates to a process for synthesis of Eliglustat and pharmaceutically acceptable salts thereof, and relates to the intermediate compounds in the process and a process for preparation of the intermediate compounds.
专利号:US-9233943-B2 优先权日:2012-01-10 标题:Process for synthesis of syn azido epdxide and its use as intermediate for the synthesis of amprenavir and saquinavir 发明人:GADAKH SUNITA KHANDERAO; REKULA REDDY SANTHOSH; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:A novel synthetic route to the syn-azido epoxide of formula 5 includes cobalt-catalyzed hydrolytic kinetic resolution of a racemic mixture of the azido-epoxide. Reaction steps include subjecting an allylic alcohol to epoxidation with mCPBA to obtain a racemic epoxy alcohol; ring opening the epoxy alcohol with azide anion to obtain an anti-azido alcohol, which can then be selectively tosylated at the primary alcohol; treating the tosylate with base to obtain the racemic azido-epoxide; and subjecting the racemic azido-epoxide to cobalt-catalyzed hydrolytic kinetic resolution to obtain the syn-azido epoxide of formula 5. The compound of formula 5 may be used as a common intermediate for the asymmetric synthesis of HIV protease inhibitors, such as Amprenavir, Fosamprenavir, Saquinavir, and formal synthesis of Darunavir and Palinavir.
专利号:US-6639059-B1 优先权日:1999-03-24 标 题 :Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.
专利号:US-6734291-B2 优先权日:1999-03-24 标题:Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs
专利号:US-5545568-A 优先权日:1992-09-14 标题:Solid phase and combinatorial synthesis of compounds on a solid support 发明人:ELLMAN JONATHAN A 权利人:UNIV CALIFORNIA 摘要:Methods, compositions, and devices for synthesizing combinatorial libraries of various useful compounds, such as benzodiazepines, prostaglandins, β-turn mimetics and glycerol-derived drugs is described. In order to expediently synthesize such combinatorial libraries of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. This disclosure thus also describes an important extension of solid phase synthesis methods to nonpolymeric organic compounds.
专利号:US-6891033-B2 优先权日:2001-01-31 标题:Labelling compounds for the simple synthesis of 3'-[18F]fluoro-3'-deoxythymidine and a method for the production thereof 发明人:MARTIN STEFAN JOHANNES; EISENBARTH JOSEPH ANTONIUS MAR; WAGNER-UTERMANN ULRIKE; EISENHUT MICHAEL; MIER WALTER 权利人:DEUTSCHES KREBSFORSCH 摘要:The application relates to compounds that are suitable as labelable precursors for synthesis of 3′-[ 18 F]fluoro-3′-deoxythymidine and that have formula (1), n n nin whichn R denotes triphenylmethyl, triphenylmethyl substituted in the phenyl group, trialkylmethyl, triphenylsilyl, triphenylsilyl substituted in the phenyl group, or trialkylsilyl, R′ denotes R 1 —SO 2 , where R 1 is an unsubstituted or substituted C 1 to C 5 alkyl or an unsubstituted or substituted phenyl, and R″ denotes C 2 to C 10 alkyloxycarbonyl, with the exception of 3-N-Boc-1-(3-O-nosyl-5-O-trityl-2-deoxy-β-D-lyxofuranosy nn The application also relates to a method for preparation of these compounds and to the use of the same for synthesis of 3′-[ 18 F]fluoro-3′-deoxythymidine.
参考标题:The Organocatalytic Synthesis Of Perfluorophenylsulfides Via The Thiolation Of Trimethyl(Perfluorophenyl)Silanes And Thiosulfonates 作者:Jinyun Luo,Muze Lin,Leifang Wu,Zhihua Cai,Lin He,Guangfen Du 摘要:The Organic Superbase T-Bu-P4-Catalyzed Direct Thiolation Of Trimethyl(Perfluorophenyl)Silanes And Thiosulfonates Was Developed. Yields Of Perfluorophenylsulfides Of Up To 97% Under Catalysis Of 5 Mol% T-Bu-P4 Were Achieved. This Method Was Shown To Provide An Efficient Way To Construct The Perfluorophenyl-Sulfur Bond Under Mild Metal-Free Reaction Conditions.
合成参考文献
参考文献:10.1107/s1600536811017818 摘要:Uludağ N, Ateş M, Tercan B, Hökelek T. 9-(4-Nitro-phenyl-sulfon-yl)-9H-carbazole. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1428–9.