(R)-Flurbiprofen, MPC-7869, E-7869, Flurizan
(R)-氟比洛芬(Tarenflurbil)Chemical Name: 2(R)-(2-Fluorobiphenyl-4-yl)propionic acid
CAS No. 51543-40-9
项目整合开发状态: Phase II/III
项目研究机构: Encore (Originator), Loma Linda University (Originator), Myriad Genetics (Licensee)
合成路线:Formation of the diastereoisomeric salts with (R)-alpha-methylbenzylamine (II),followed by crystallization from methanol/toluene,provided the desired (R)-phenylpropionic acid salt (III) in good enantiomeric purity,which was further enriched in the desired enantiomer by recrystallization from the same solvent.The chiral carboxylic acid was then liberated from the recrystallized methylbenzylamine salt (III) by acidification with HCl in a water/heptane two-phase system.
📌 参考资料/链接：
参考文献标题:Process for preparing substantially pure enantiomers of phenylpropionic acids
文献作者:Coe,P.F.; Hardy,R.; Hirst,A.; O'Donnell,H.O.(The Boots Company plc)
参考来源:WO 9412460
📄 详细内容
合成路线:A different synthetic process consisted in the asymmetric olefin hydroformylation of 2-fluoro-4-vinylbiphenyl (IV) using a Rh4(CO)12 in the presence of the chiral catalyst (2R,4R)-di[2,2'-(3,3'-di-tert-butyl-5,5'-dimethoxy-1,1'-biphenyl)]-2,4-pentyl diphosphite under a pressurized atmosphere of CO/H2.The resultant chiral aldehyde (V) was further oxidized to the corresponding carboxylic acid employing several different oxidant reagents.
参考文献标题:Process for preparing optically active carboxylic acids
文献作者:Barner,B.A.; Kurland,J.J.
参考来源:WO 9714669
产品链接: CAS No. 51543-40-9››