专利号:US-8101779-B2 优先权日:2008-10-06 标题 :Enantioselective synthesis of (+) and (–)-2-[1-(2,6-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene 发明人:CROOKS PETER A; VARTAK ASHISH PRAMOD 权利人:CROOKS PETER A; VARTAK ASHISH PRAMOD; UNIV KENTUCKY RES FOUND 摘要:Methods for the enantioselective synthesis of (+) and (−) lofexidine or 2-[1-(2,6)-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene involve converting (+) or (−) 1-methyl-1-[2,6-dichlorophenoxy]ethanamide to an (+) or (−) imino-ether intermediate by electrophilic attack of the amide oxygen by a trimethoxonium ion and, without isolation, converting the (+) or (−) imino-ether intermediate to (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene by adding ethylene diamine; and optionally converting the (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene into a pharmaceutically acceptable acid addition salt thereof.
专利号:US-2009162290-A1 优先权日:2005-09-09 标 题 :Method for the synthesis of penta-pendant enantiomer-pure chelators and process for therapeutically active bioconjugates preparation by a covalent binding thereof 发明人:BENES IVAN; CIHELNIK SIMON; DROZ LADISLAV; SRAMEK MARTIN 权利人:THERAPHARM GMBH 摘要:The present invention provides a method for synthesis and binding methods of pentapendant enantiomer-pure chelators of formula (VII) wherein R 1 , R 2 , R 3 , R 4 are groups forming an adequate enantiomer of the chelator; and X 1 -X 5 , Y 1 -Y 5 , Z 1 -Z 5 each individually forming pendant chelating groups.
专利号:US-2024368343-A1 优先权日:2021-08-26 标题:Valorisation of d-lactic acid stream in the production process of l-polylactic acid 发明人:COSZACH PHILIPPE; VAN GANSBERGHE MARTIN 权利人:FUTERRO SA 摘要:The present invention discloses a valorization method of a flux containing undesired D-lactic acid (ester(s)) in the production process of L-polylactic acid, the production thereof comprising: oligomerisation (30) of a substantially pure L-lactic acid feed; cyclisation (40) of the lactic acid oligomers, thereby obtaining lactides and a first residual stream transferred, at least partially, to a transesterification (80) and a hydrolysis (90) step; lactide purification (50), thereby obtaining purified lactides comprising L-lactide and meso-lactide, a second and a third residual stream, wherein the second residual stream is transferred, at least partially, to the oligomerisation (30) step and the third residual stream is transferred, at least partially, to a transesterification (80) and a hydrolysis step (90); polymerisation (60) of the purified lactides into poly lactic acid; purification (70) of the poly lactic acid, thereby obtaining purified polylactic acid comprising substantially L-polylactic acid and unreacted L-lactide, unreacted meso-lactide and impurities transferred, at least partially, to the lactide purification step (50); transesterification (80) and hydrolysis (90) of the at least partially transferred first and third residual streams, thereby obtaining a fourth and a fifth residual stream which are used, at least partially, as a base for the synthesis of molecules insensitive to the optical isometry D or L of lactic acid (esters).
专利号:US-2004249147-A1 优先权日:2001-09-25 标题:Synthesis of key azole-antifungal intermediates 发明人:SATTIGERI JITENDRA; ARORA JASBIR SINGH; MALHOTRA SANJAY; VERMA ASHWANI KUMAR; SALMAN MOHAMMAD 摘要:Methods for producing azole compounds useful as intermediates for antifungal compounds and compositions including reaction of epoxy alcohols with reactants having active hydrogen attached to nitrogen, oxygen or sulfur in the presence of redox coupling agents. In some embodiments, a procedure known as a Mitsunobu reaction is utilized for the transformations.
专利号:US-11352311-B1 优先权日:2021-06-27 标题:Single-step stereospecific synthesis of (S)-2-chloropropionic acid alkyl ester 发明人:PATEL-FRAMROZE BOMI 权利人:PATEL FRAMROZE BOMI 摘要:Provided herein is a process to react optically pure alkyl lactates with thionyl chloride in the presence of a catalytic amount of a lewis base ionic liquid to produce optically pure chloropropionic acid alkyl esters.
专利号:WO-9967219-A1 优先权日:1998-06-22 标 题:Compounds for inhibiting beta-amyloid peptide release and/or its synthesis 发明人:AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING 权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING 摘要:Compounds of formula (I), wherein W is a cyclic group of the type (2); (3); Y is represented by the formula (II); these compounds inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising 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.
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合成参考文献
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