专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
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-2011113486-A1 优先权日:2010-03-17 标 题 :Process for the synthesis of hydroxyphenylglycine esters 发明人:PALLARES BAYO ANTONIO; LOPEZ SANCHEZ RAMON; SANTIANDREU LOPEZ RICARDO MANUEL 权利人:DERETIL S A; PALLARES BAYO ANTONIO; LOPEZ SANCHEZ RAMON; SANTIANDREU LOPEZ RICARDO MANUEL 摘要:The present invention refers to a process for the synthesis of a D-(-)-p-hydroxyphenylglycine (HPG) ester in crystal form, by crystallizing D-HPG ester from a solution containing dissolved D-HPG ester to obtain a suspension comprising D-HPG ester crystals, characterized in that the ee D of the D-HPG ester in the solution and the ee D of the D-HPG ester crystals is above 95%, preferably above 97%, more preferably above 98%, more preferably above 99%, more preferably above 99.5%.
专利号:WO-2005100367-A1 优先权日:2004-04-13 标 题 :Intermediates useful in the synthesis of 3-(2-substituted vinyl) cephalosporins 发明人:KUMAR YATENDRA; PRASAD MOHAN; SINGH KAPTAN; PRASAD ASHOK; RICHHARIYA SANTOSH 权利人:RANBAXY LAB LTD; KUMAR YATENDRA; PRASAD MOHAN; SINGH KAPTAN; PRASAD ASHOK; RICHHARIYA SANTOSH 摘要:The present invention relates to crystalline intermediates useful in the synthesis of 3-(2-substituted vinyl) cephalosporins and processes for their preparation. In particular, the present invention relates to crystalline ylides of Formula I, processes for their preparation, and their use as an intermediate in thepreparation of 3-(2-substituted vinyl) cephalosporins.
专利号:US-2003044884-A1 优先权日:2000-10-11 标题:Synthesis of beta-lactam antibacterials using soluble side chain esters and enzyme acylase 发明人:USHER JOHN J; ROMANCIK GUNA 摘要:Disclosed is a process for the synthesis of β-lactam antibacterials using soluble side chain esters in the presence of enzyme acylase. Also disclosed are novel esters useful as reactants in said process.
专利号:US-2005186197-A1 优先权日:2002-08-29 标 题:Peptide inhibitors of beta lactamases 发明人:PALZKILL TIMOTHY; HUANG WANZHI 摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.
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