Cobalt-promoted regioselective preparation of aryl tetrazole amines

Regioselective Annulation of Aryl Sulfonamides with Allenes through Cobalt-Promoted C-H Functionalization.

The development of an efficient method for the construction of biologically relevant sultams is described, which represents the first case of cobalt-promoted C-H/N-H functionalization of sulfonamides with allenes. This newly developed annulation reaction demonstrated good functional group tolerance and excellent regioselectivity. Both terminal monosubstituted allenes and internal disubstituted ...

N-Aryl Lactams by Regioselective Ozonation of N-Aryl Cyclic Amines

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 func...

Microwave Irradiation Promoted Reactions of Benzoxazin-4-Ones with Primary Amines. Preparation of 4(2=3H)-Quinazolinones

An efficient synthesis of 3-substituted or 2,3-disubstituted 4(3H)-quinazolinones from benzoxazin-4-ones and primary amines under microwave irradiation in unsealed vessels is described.

Base-promoted aryl-bromine bond cleavage with cobalt(II) porphyrins via a halogen atom transfer mechanism.

Aryl-bromine bonds are successfully cleaved by cobalt(II) porphyrins in basic media to give Co(por)Ar (por = porphyrin) in good yields. Mechanistic studies suggested that the aryl-bromine bond is cleaved through a halogen atom transfer mechanism, which is different from the aryl-halogen bond cleavage mechanism with other group 9 metalloporphyrins.

General preparation of primary, secondary, and tertiary aryl amines by the oxidative coupling of polyfunctional aryl and heteroaryl amidocuprates.