Ozonation of N-aryl-cyclic amines in organic solvents gave N-aryl-lactams regioselectively. In particular, 4-(4-aminophenyl)-morpolin-3-one, a key intermediate in the preparation of factor Xa inhibitors, was obtained in fair yields. The method represents an alternative approach for the lactamization of tertiary N-arylic substrates and is based on a “metal-free” introduction of the carbonyl function into the heterocyclic ring.
Saliu, F., Orlandi, M., Bruschi, M. (2012). N-Aryl Lactams by Regioselective Ozonation of N-Aryl Cyclic Amines. ISRN ORGANIC CHEMISTRY, 2012, 1-5 [10.5402/2012/281642].
N-Aryl Lactams by Regioselective Ozonation of N-Aryl Cyclic Amines
SALIU, FRANCESCO;ORLANDI, MARCO EMILIO;BRUSCHI, MAURIZIO
2012
Abstract
Ozonation of N-aryl-cyclic amines in organic solvents gave N-aryl-lactams regioselectively. In particular, 4-(4-aminophenyl)-morpolin-3-one, a key intermediate in the preparation of factor Xa inhibitors, was obtained in fair yields. The method represents an alternative approach for the lactamization of tertiary N-arylic substrates and is based on a “metal-free” introduction of the carbonyl function into the heterocyclic ring.
File in questo prodotto:
Non ci sono file associati a questo prodotto.
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
