ASYMMETRIC FORMAL SYNTHESIS OF(-)-FORMOTEROL AND(-)-TAMSULOSIN

摘要

Biologically important(2R)-2-amino-3-phenylpropanes consisted in commercial drugs including(R,R)-formoterol,and(R)-tamsulosin were prepared from chiral(2R)-aziridine-2-carboxylate without any chromatographic separation.Key reactions include regio-and stereoselective ring opening reaction of aziridin-2-yl-phenylmethanol and subsequent cyclization toward enantiopure 4,5-disubastitued oxazolidin-2-ones as synthetic intermediates.