3-(Methanesulfonyl)-2-Azabicyclo<2.2.1>Hepta-2,5-Diene置于溶剂黄146体系中,用 二氯甲烷 作为反应溶剂,化学反应 1.0H,反应生成 2-氮杂双环[2.2.1]庚-5-烯-3-酮 参考文献:Diels-Alder Reaction Of Methanesulfonyl Cyanide With Cyclopentadiene. Industrial Synthesis Of 2-Azabicyclo[2.2.1]Hept-5-En-3-One 标题:Diels-Alder Reaction Of Methanesulfonyl Cyanide With Cyclopentadiene. Industrial Synthesis Of 2-Azabicyclo[2.2.1]Hept-5-En-3-One 摘要: DOI:10.1021/jo00074A050
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-10975096-B2 优先权日:2014-06-20 标题 :Synthesis of polycyclic-carbamoylpyridone compounds 发明人:CHIU ANNA; ENQUIST JR JOHN; GRIGGS NOLAN; HALE CHRISTOPHER; IKEMOTO NORIHIRO; KEATON KATIE ANN; KRAFT MATT; LAZERWITH SCOTT E; LEEMAN MICHEL; PENG ZHIHUI; SCHRIER KATE; TRINIDAD JONATHAN; VAN HERPT JOCHEM; WALTMAN ANDREW W 权利人:GILEAD SCIENCES INC 摘要:Methods of making compounds of Formula I are disclosed:
专利号:US-5284769-A 优先权日:1989-10-16 标题 :Process for preparing a single enantiomer of a lactam using lactamase 发明人:EVANS CHRISTOPHER T; ROBERTS STANLEY M 权利人:CHIROS LTD 摘要:Lactams of 1-amino-3-carboxylic acid cyclic compounds are produced in enantiomeric form, together with an enantiomer of the corresponding ring-opened amino-acid or ester, by reaction of the racemic lactam with a novel lactamase. The products are useful in the synthesis of chiral carbocyclic nucleotides.
专利号:US-2010204463-A1 优先权日:2007-08-07 标题 :Preparation Of Synthetic Nucleosides via Pi-Allyl Transition Metal Complex Formation 发明人:LIOTTA DENNIS C; LI YONGFENG 权利人:LIOTTA DENNIS C; LI YONGFENG 摘要:This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof.
专利号:US-5300649-A 优先权日:1991-09-12 标 题 :Process for the production of lactams 发明人:GRIFFITHS GARETH DR; PREVIDOLI FELIX DR 权利人:LONZA AG 摘要:β,γ-unsaturated δ-lactams, especially 2-azabicyclo[2.2.1]hept-5-en-3-one, are produced by Diels-Alder reaction of 1,3-dienes with sulfonyl cyanides and subsequent hydrolysis. The sulfonyl cyanides were formed in situ from cyanogen chloride and the corresponding sulfinates. By the renewed reaction of the sulfinate formed in the hydrolysis of the Diels-Alder adducts with cyanogen chloride, the sulfonyl cyanides are regenerated and a catalytic cyclic process results. The 2-azabicyclo[2.2.1]hept-5-en-3-one is a starting compound in the synthesis of antiviral nucleoside analogs.
专利号:US-7358073-B2 优先权日:1997-11-27 标题:Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4(2-amino-6-chloro-5-formamido-4- pyrimidinyl)-amino-2-cyclopentenyl-1-methanol 发明人:BRIEDEN WALTER; SCHROER JOSEF; BERNEGGER-EGLI CHRISTINE; URBAN EVA MARIA; PETERSEN MICHAEL; RODUIT JEAN-PAUL; BERCHTOLD KATJA; BREITBACH HOLGER 权利人:LONZA AG 摘要:The invention relates to a novel process for the preparation of an aminoalcohol of the formula n nracemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulaen n nIn the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) formamide of the formulan n nto give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulaen n nand then cyclized to give the end compounds.