专利号:US-4837355-A 优先权日:1980-08-21 标 题:Process for the synthesis of phenoxyalkane derivatives 发明人:WATSON KEITH G 权利人:ICI AUSTRALIA LTD 摘要:The invention concerns a process for the synthesis of a compound of formula I ##STR1## wherein: U and V may be chosen from a range of substituents including hydrogen, halogen, alkyl and alkoxy; R 1 and R 2 may be chosen from a range of substituents including hydrogen and alkyl; n is 0, 1 or 2; and W may be chosen from a range of substitutents including the group ##STR2## which may be a free carboxylic acid or derivative thereof; the process comprising reacting a sulfate ester of formula II, wherein Q is a cation, with a compound of formula III, wherein L is a leaving group ##STR3## and hydrolyzing the sulfate ester formed. Preferably the sulfate ester of formula II is prepared by the oxidation of a phenol of formula IV with a persulfate. ##STR4##
专利号:US-6235899-B1 优先权日:1997-07-15 标 题 :Method for preparing alkyloxy furanone derivatives, compounds obtained by said method and use of said compounds 发明人:BOUCHET RAPHAEL; BRION FRANCIS; COLLADANT COLETTE; LAGOUARDAT JACQUES 权利人:HOECHST MARION ROUSSEL INC 摘要:The invention relates to a novel process for preparing compounds of the formula (IV) or (I):from the racemic alkoxyfuranone of the formula (II):R1 and R2 being as defined in the description, to the novel compounds of the formula (IV) as well as to the intermediate compounds of this process, and to the use of the compounds of the formula (IV) or (I) in the process for the synthesis of compounds which inhibit interleukin-1beta converting enzyme.
专利号:WO-2011158257-A1 优先权日:2010-06-18 标题 :Preparation process of fesoterodine and intermediates 发明人:JAIN RAJESH; RAO SIRIPRAGADA MAHENDER; RAO JAGADEESHWAR R; MADADA CHANDRA RAO 权利人:PANACEA BIOTEC LTD; JAIN RAJESH; RAO SIRIPRAGADA MAHENDER; RAO JAGADEESHWAR R; MADADA CHANDRA RAO 摘要:The present invention relates to a process of synthesis of 3,3 dipheylpropylamines, which may be used as pharmaceutical intermediates in the preparation of their pharmacologically active derivatives such as fesoterodine, tolterodine, their enantiomers, pharmaceutically acceptable salts and related compounds useful as antimuscarinic agents.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 权利人:LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
[参考文献]: Ye Yuan, Et Al. Metabolic Fate Of The (14)C-Labeled Herbicide Clodinafop-Propargyl In A Sediment-Water System. J Environ Sci Health B. 2015;50(8):533-43.