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.
Articolo in rivista - Articolo scientifico
ozone, N-aryl-lactams
English
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5
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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].
Saliu, F; Orlandi, M; Bruschi, M
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/38056
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