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-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
专利号:US-9334273-B1 优先权日:2014-03-05 标题:Efficient and stereoselective synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) 发明人:CHU DAVID C K; SINGH UMA S 权利人:UNIV GEORGIA 摘要:The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) from a readily available starting material (Vince lactam) in fourteen steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, D -2′-fluoro-6′-methylene cyclopentanol by diazotization, elimination, stereoselective epoxidation, fluorination and oxidative reduction of the Vince lactam in twelve steps is also provided.
专利号:US-6818633-B2 优先权日:2001-06-29 标题:Antiviral compounds and methods for synthesis and therapy 发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
专利号:US-2015376219-A1 优先权日:2014-06-30 标题 :Selective Preparations of Purine Nucleosides and Nucleotides: Reagents and Methods 发明人:ZHONG MINGHONG 权利人:ZHONG MINGHONG 摘要:A process of regiospecific synthesis of N-9 purine nucleoside analogs in either solution or solid phase synthesis is described. The introduction of the sugar moiety or its analogue on to a 6-heteroarylium purine or its mesomeric betaine so that formation of only the N-9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific introduction of the sugar moiety allows the synthesis of purine nucleoside analogs in high yields without formation of the N-7-positional regioisomers, while the 6-heteroaryliums are leaving groups facilitated for nucleophilic displacement. Solid supported 6-heterarylium purine bases can be used for purine based library synthesis and synthesis of nucleotide monophosphates and polyphosphates. Processes for providing novel 6-heteroarylium purines and their corresponding mesomeric betaines for the regiospecific synthesis of N-9 purine nucleoside analogs and nucleotides are described.
专利号:US-2010261876-A1 优先权日:2007-09-25 标 题:Novel methods of synthesis for therapeutic antiviral peptides 发明人:BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E 权利人:BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E 摘要:Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.