81937-33-9Relevant articles and documents
Preparation method of flurbiprofen
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Paragraph 0024; 0028; 0030, (2021/01/29)
The invention discloses a preparation method of flurbiprofen. The method comprises the following steps: adding 2-(3-fluoro-4-bromophenyl)propionic acid and phenylboronic acid into a water-system solvent under alkaline conditions, and carrying out a palladium-carbon catalyzed coupling reaction to obtain flurbiprofen. The method has the advantages that operation is simpler, the prepared flurbiprofenis higher in purity, industrialized production is facilitated.
Preparation of optically pure flurbiprofen via an integrated chemo-enzymatic synthesis pathway
Enoki, Junichi,Linhorst, Max,Busch, Florian,Baraibar, álvaro Gomez,Miyamoto, Kenji,Kourist, Robert,Mügge, Carolin
, p. 135 - 142 (2019/02/14)
In the synthesis of chiral molecules, the incorporation of enantioselective enzymatic conversions within the synthetic route often presents a useful approach. For the substitution of a chemical step with an enzymatic reaction, however, the complete synthetic route leading to and from this reaction needs to be considered carefully. An integrated approach, taking the possibilities and challenges of both types of conversions into account, can give access to chemo-enzymatic processes with great potential for effective synthesis strategies. We here report on the synthesis of enantiopure flurbiprofen using arylmalonate decarboxylase (AMDase, EC 4.1.1.76) in a chemo-enzymatic approach. Interestingly, practical considerations required shifting the enzymatic step to an earlier position in the synthetic route than previously anticipated. Engineered enzyme variants made it possible to obtain both (R)- and (S)-enantiomers of the target compound in excellent optical purity (>99%ee). The presented results underline that enzymes are most useful when they fit in a synthetic route, and that the optimization of biocatalytic steps and the planning of synthetic routes should be an integrated process.
Novel styrene derivatives of the general formula
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, (2008/06/13)
Novel styrene derivatives of the general formula STR1 wherein X is hydrogen or halogen, X1 is halogen, R is hydrogen or methyl, Y is hydroxymethyl, carboxyl, --COOR1 or --COR2 wherein R1 is prenyl, geranyl, farn