6-溴己酸甲酯置于六甲基磷酰三胺,Lithium Diisopropyl Amide体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 环戊烷甲酸甲酯 参考文献:The Synthesis Of A β-Methylene-γ-Spirolactone 标题:The Synthesis Of A β-Methylene-γ-Spirolactone 摘要: DOI:10.1055/s-1977-24286
专利号:US-2006051291-A1 优先权日:2004-09-07 标题 :Synthesis of radiolabeled sugar metal complexes 发明人:ADAM MICHAEL J; FISHER CARA L; BAYLY SIMON R; ORVIG CHRISTOPHER; LIM NATHANIEL C; STORR TIMOTHY J; EWART CHARLES B 权利人:ADAM MICHAEL J; FISHER CARA L; BAYLY SIMON R; ORVIG CHRISTOPHER; LIM NATHANIEL C; STORR TIMOTHY J; EWART CHARLES B 摘要:The invention provides a method for manufacturing or preparing neutral, low molecular weight 99m Tc-labeled and 186 Re-labeled carbohydrate complexes with an improved radiochemical yield from a simple functionalized sugar, such as glucosamine. In particular the synthesis relies on single ligand transfer (SLT) or double ligand transfer (DLT) reactions for converting a ferrocene compound into a rhenium or technetium tricarbonyl complex. The ferrocene compound may be linked to a sugar through various functional groups including, for example, thio, amino and alcohol functionalities to provide a wide range of radiolabeled sugar complexes that include both water soluble and relatively water insoluble compounds.
专利号:US-2023303611-A1 优先权日:2022-01-21 标题:Synthesis of an antiviral azasugar triphosphate 发明人:KOTIAN PRAVIN L; Dang zhao; WU MINWAN 权利人:BIOCRYST PHARM INC 摘要:Provided are methods of making the active 5′-triphosphate form of galidesivir (compound 1) and the active 5′-triphosphate form of azasugar nucleoside analogues (compound 2):a potent anti-viral compound useful for broad spectrum treatment, suppression, and prevention of viral infections. The syntheses of compound 1 and compound 2 can be achieved via selective formation of protected intermediate 1b and protected intermediate 2b, respectively:
专利号:EP-2097079-B1 优先权日:2006-11-30 标题:Modulation of prostaglandin/cyclooxygenase metabolic pathways 发明人:WUELFERT ERNST 权利人:HUNTER FLEMING LTD 摘要:A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2. The compounds are 7-hydroxy-steroids or condensed indoles.
专利号:US-5942632-A 优先权日:1995-07-28 标题:Solid phase synthesis method 发明人:WANG GARY T 权利人:ABBOTT LAB 摘要:A solid phase synthesis method and intermediates useful in the process are disclosed for the preparation of diamino diol and diamino alcohol inhibitors of HIV protease.
专利号:US-4810778-A 优先权日:1986-01-16 标 题 :Intermediates for preparing 1,6-dicarba-vasopressin compounds 发明人:CALLAHAN JAMES F; HUFFMAN WILLIAM F; NEWLANDER KENNETH A; YIM NELSON C F 权利人:SMITHKLINE BECKMAN CORP 摘要:New compounds which have potent V2-vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by the Pas1,6 or Tas1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.
专利号:US-5827855-A 优先权日:1992-12-28 标题 :Hexahydronaphthalene ester derivatives their preparation and their therapeutic uses 发明人:KOGEN HIROSHI; ISHIHARA SADAO; KOGA TEIICHIRO; KITAZAWA EIICHI; SERIZAWA NOBUFUSA; HAMANO KIYOSHI 权利人:SANKYO CO 摘要:Compounds of formula (I): (I) wherein R1 represents a group of formula (II) or (III): (II) (III) R2 is alkyl, alkenyl or alkynyl; R3 and R4 are each hydrogen, alkyl, alkenyl or alkynyl; R5 is hydrogen or a carboxy-protecting group; Ra is a group of formula -OR6; R6 is hydrogen; R6a and R6b are each hydrogen, a hydroxy-protecting group, alkyl, alkanesulfonyl, halogenated alkanesulfonyl or arysulfonyl, and their salts and esters. Such compounds inhibit the synthesis of cholesterol, and can be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.