On water N -arylation of oxetanylamines for the preparation of N -aryl-oxetanylamines; potentially useful aryl-amide isosteres

Maud Bollenbach , William Lecroq , Patrick Wagner (1) , Thomas Fessard , Martine Schmitt (1) , Christophe Salomé (1)

1 LIT - Laboratoire d'Innovation Thérapeutique

A Pd cross-coupling approach for the synthesis of N-aryl-oxetanyl-amines has been developed. This method provides new building blocks potentially useful in medicinal chemistry as amide bioisosteres. The reactions are conducted in water employing the renewable feedstock surfactant TPGS-750-M.

Domaines: Catalyse; Chimie organique

Maud Bollenbach, William Lecroq, Patrick Wagner, Thomas Fessard, Martine Schmitt, et al.. On water N -arylation of oxetanylamines for the preparation of N -aryl-oxetanylamines; potentially useful aryl-amide isosteres. Chemical Communications, 2019, 55 (11), pp.1623-1626. ⟨10.1039/c8cc09110b⟩. ⟨hal-02322869⟩