专利号:WO-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:WO-2006109321-A1 优先权日:2005-04-15 标题:An improved process for the synthesis of palmidrol 发明人:SURI SANJAY; KASHYAP TAPAN; SINGH JAGAT 权利人:MOREPEN LAB LTD; SURI SANJAY; KASHYAP TAPAN; SINGH JAGAT 摘要:The process of this invention comprises preparing anhydride of palmitic acid and alkyl or cycloalkyl haloformate by any conventional method, reacting anhydride so formed with ethnolamine in-situ, and isolating the product by any known methods such as solvent recovery or filtration followed by purifying the title product by recrystallization using organic solvents if so desired.
专利号:US-5254558-A 优先权日:1991-08-15 标 题:Substituted 1,3-diazines as leukocyte elastase inhibitors 发明人:BERNSTEIN PETER R; EDWARDS PHILIP D; THOMAS ROYSTON M; VEALE CHRIS A; WARNER PETER; WOLANIN DONALD J 权利人:ICI PLC 摘要:The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.
专利号:US-4734495-A 优先权日:1985-07-17 标 题 :Process and intermediates for beta-lactam antibiotics 发明人:EVANS DAVID A; SJOGREN ERIC B 权利人:HARVARD COLLEGE 摘要:1-Benzyl(or substituted benzyl)-3β-[4(S)-aryloxazolidin-2-one-3-yl]-4β-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic β-lactam antibiotics.
专利号:US-4870169-A 优先权日:1985-07-17 标 题:Intermediates for beta-lactam antibiotics 发明人:EVANS DAVID A; SJOGREN ERIC B 权利人:HARVARD COLLEGE 摘要:1-Benzyl(or substituted benzyl)-3β-[4(S)-aryloxazolidin-2-one-3-yl]-4β-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic β-lactam antibiotics.
专利号:US-4665171-A 优先权日:1985-07-17 标 题:Process and intermediates for β-lactam antibiotics 发明人:EVANS DAVID A; SJOGREN ERIC B 权利人:UNIV HARVARD 摘要:1-Benzyl (or substituted benzyl)-3β-[4(S)-aryloxazolidin-2-one-3-yl]-4β-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic β-lactam antibiotics.