2-甲基-1,3-二氧戊环置于n-溴代丁二酰亚胺(Nbs),过氧化苯甲酰体系中,用 四氯化碳 作为反应溶剂,化学反应生成 2-溴乙基乙酸酯 参考文献:Gelas,J.; Michaud,S.,Bulletin De La Societe Chimique De France,1972,P. 2445-2459 标题:Gelas,J.; Michaud,S.,Bulletin De La Societe Chimique De France,1972,P. 2445-2459
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:WO-0120995-A9 优先权日:1999-09-23 标题:Compounds directed against pilus biogenesis and activity in pathogenic bacteria; methods and compositions for synthesis thereof 发明人:KIHLBERG JAN; LARSSON ANDREAS; SVENSSON ANETTE; FEX TOMAS; HULTGREN SCOTT J; PINKNER JERRY 权利人:UNIV WASHINGTON; KIHLBERG JAN; LARSSON ANDREAS; SVENSSON ANETTE; FEX TOMAS; HULTGREN SCOTT J; PINKNER JERRY 摘要:Many Gram-negative pathogens assemble adhesive structures on their surfaces that allow them to colonize host tissues and cause disease. Novel compositions which inhibit or prevent the formation of a pilus chaperone-subunit complex are disclosed. Interfering with the function of the pili chaperone negatively affects the chaperone/usher pathway which is one molecular mechanism by which Gram-negative bacteria assemble adhesive pili structures and thus prevent or inhibit pilus assembly. Also provided are methods for the treatment or prevention of diseases caused by tissue-adhering pilus-forming bacteria by inhibiting the function of pilus chaperones. Also provided are pharmaceutical preparations capable of inhibiting or preventing the formation of a pilus chaperone-subunit complex. Also provided are methods of synthesizing the N-substituted amino acid compounds and compounds useful for the synthesis thereof. In particular, novel fluorinated linker compounds and methods of synthesis are provided. Methods for using the fluorinated linker compounds in methods of solid-phase synthesis of the N-substituted amino acid compounds are also disclosed.
专利号:US-8193360-B2 优先权日:2003-07-31 标 题:Radiolabelled fluorobenzamide analogues, their synthesis and use in diagnostic imaging 发明人:MACH ROBERT H; TU ZHUDE 权利人:MACH ROBERT H; TU ZHUDE; UNIV WASHINGTON 摘要:Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18 F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123 I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
专利号:US-2004110957-A1 优先权日:2002-12-05 标 题 :Process for the synthesis of an antiviral compound 发明人:WILKEN JOERG; NERENZ FRANK; KANSCHIK-CONRADSEN ANDREAS 权利人:HONEYWELL INT INC 摘要:In a process comprising synthesizing pyranes including [R—(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide the present invention comprises the improvements comprising: (a) providing a racemic mixture of 3-hydroxy-3-(2-phenylethyl)-hexanoate ethyl acetate by reacting said 1-phenyl-hexan-3-one with ethylbromoacetate under Reformatsky conditions; and (b) separating (R)-3-hydroxy-3-(2-phenylethyl)-hexanoic acid in enantiomeric excess by saponification and reverse resolution of the racemate of step (a) to produce a resolved product. In addition, the present invention comprises a reverse resolution process for separating an enantiomer from a mixture of enantiomers.
专利号:US-2009143426-A1 优先权日:2007-12-04 标 题:Synthesis of 1,3,6-trisubstituted-2-carboxyquinol-4-ones as selective ET A antagonists and their use as medicaments 发明人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 权利人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 摘要:The invention discloses the composition and preparation of various 1,3,6-trisubstituted-2-carboxy-quinol-4-ones of the formula 1 where R is H, alkyl, haloalkyl or hydroxyalkyl, R′ is alkyl, nitro, halogen or NR 2 ′″ where R′″ is alkyl or cycloalkyl, and R″ is H or alkyl. The composition of the invented compounds as methods of antagonizing the action of endothelin-1 to treat cardiovascular, pulmonary diseases and obstetric disorders and preterm labor and preeclampsia in mammals is disclosed.
专利号:US-6262272-B1 优先权日:1997-11-13 标题 :Method of synthesis of pyrrole amides 发明人:RAGAN JOHN ANTHONY; MAKOWSKI TERESA WOODALL; AM ENDE DAVID JON; CLIFFORD PAMELA JANE; YOUNG GREGORY RANDALL; CONRAD ALYSON KAY; EISENBEIS SHANE ALLEN; QUALLICH GEORGE JOSEPH; ALLEN DOUGLAS JOHN MELDRUM 权利人:PFIZER 摘要:A method for preparing pyrrole-carboxyamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloakane-diones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.
摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 76. 摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 38. 摘要:Molander, G. A.; Beaumard, F., Science of Synthesis Knowledge Updates, (2013) 3, 131. 摘要:Wolf, C., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 875.