专利号:US-8889897-B2 优先权日:2011-12-23 标 题:Electrocarboxylation synthesis for obtaining intermediates useful for the synthesis of SPAN derivatives 发明人:OSSO J ORIOL; VEGA LOURDES F; GALLARDO ILLUMINADO; GUIRADO GONZALO; GOMEZ ANA BELEN; RECHE FRANCISCA IRENE 权利人:AIR PROD & CHEM 摘要:The present invention relates to a process for obtaining a compound of formula (1), (2) or (3) by means of a electrocarboxylation with CO 2 . The present invention also relates to the new intermediates (1) and (2). The present invention further relates to the use of intermediates (1) and (2) as starting materials for the synthesis of SPAN derivatives.
专利号:US-8426630-B2 优先权日:2009-08-31 标题:Method and apparatus for continuous flow synthesis of ibuprofen 发明人:MCQUADE D TYLER; BOGDAN ANDREW; POE SARAH LIHOA 权利人:MCQUADE D TYLER; BOGDAN ANDREW; POE SARAH LIHOA; UNIV FLORIDA STATE RES FOUND 摘要:A multi-step method for the continuous synthesis of ibuprofen or a synthetic precursor of ibuprofen is provided that does not require any intermediate purification or isolation steps and uses reagents compatible with downstream reactions. According to some embodiments, a method is provided wherein isobutylbenzene and a propionyl compound may be converted into a first product in a first Friedel Crafts acylation reaction. The first product may then be converted into a second product in a 1,2-aryl migration reaction. Finally, the second product may be converted into ibuprofen in a hydrolysis reaction. The present invention also provides a method wherein only the first and second reaction steps or only the second and third reaction steps are performed. An apparatus is also provided having two or more microreactors and two or more junctions in particular arrangements for the synthesis of ibuprofen or a synthetic precursor of ibuprofen.
专利号:US-5248815-A 优先权日:1991-12-27 标 题 :Stereo-selective synthesis of 2-aryl-propionic acids of high optical purity by using chiral oxazolines 发明人:PARADIES HENRICH H 权利人:PARADIES HENRICH H 摘要:The present invention relates to a stereospecific chemical synthesis of optically pure enantiomers of 2-aryl-alkanoic acids, especially those of the biologically active (S)-aryl-propionic acids, in good chemical yields, useful for preparing large quantities thereof, and having a high optical purity.
专利号:US-6175020-B1 优先权日:1999-04-09 标题 :Spirodiamino acid scaffold for combinatorial synthesis 发明人:DOLLE III ROLAND ELLWOOD; BARDEN MICHAEL C 权利人:PHARMACOPEIA INC 摘要:Azaspirononanes of formula I and their synthesis n are disclosed. The compounds are useful as templates for constructing synthetic receptors and as intermediates in the synthesis of enzyme inhibitors. They are prepared by an intramolecular ylide cycloaddition of a 6-hydrazone of 2,10-undecadienoic acid ester.
专利号:US-2015148524-A1 优先权日:2012-07-06 标题:Amino acid analogues and methods for their synthesis 发明人:WANG ZHEN; ROBINSON ANDREA; SPICCIA NICOLAS DANIEL; JACKSON WILLIAM ROY 权利人:UNIV MONASH 摘要:A method for the synthesis of an amino acid analogue or a salt, solvate, derivative, isomer or tautomer thereof comprising the steps of: (i) subjecting an amino acid containing a metathesisable group to metathesis with a compound containing a complementary metathesisable group of formula (I) or (II): (Formulae (I), (II)) wherein R 1 and R 2 are independently selected from H and substituted or unsubstituted C 1 to C 4 alkyl; each R 3 is either absent or independently selected from a heteroatom, a substituted or unsubstituted C 1 to C 20 alkyl, and a substituted or unsubstituted C 1 to C 20 alkyl group interrupted by one or more heteroatoms; and each X is independently selected from H and an effector molecule; in the presence of a reagent to catalyse the metathesis to form a dicarba bridge between the amino acid containing a metathesisable group and the compound containing a complementary metathesisable group; and (ii) reducing the dicarba bridge to form a saturated dicarba bridge, wherein the reagent used to catalyse step (i) also catalyses step (ii).
专利号:WO-0034289-A1 优先权日:1998-12-08 标 题:Process of preparing esters of penicillanic acid sulfoxide 发明人:GARDNER JOHN PAUL; ZHANG TONY YANTAO 权利人:LILLY CO ELI; GARDNER JOHN PAUL; ZHANG TONY YANTAO 摘要:A new synthesis of penicillanic sulfoxide acid ester is claimed. The synthesis starts with 6-amino penicillanic acid and proceeds through conversion to a bromide via diazotization, esterification, reduction of the bromide, and oxidation of the resulting penicillanic ester.