Potential GABA_B Receptor Antagonists. IV. Synthesis of 1-[2-Amino-1-(4-chlorophenyl)ethyl]-3-oxo-1,3-dihydro-isobenzofuran-1-yl phosphonic Acid

Abstract

The diastereoselective addition of dimethyl 3-oxo-1,3-hydroisobenzofuran-1-ylphosphonate to nitrostyrene and p- chloronitrostyrene is reported, as is the subsequent conversion of the Michael adducts into 1-[2-amino-1-phenylethyl]-3-oxo-1,3-dihydroisobenzofuran-1-ylphosphonic acid, and 1-[2-amino-1-(4-chlorophenyl)ethyl]-3-oxo-1,3 dihydroisobenzofuran-1-ylphosphonic acid respectively.