As the process for azetidine bis-arylation through coupling strategies led to a library of widely functionalized molecules, we next aimed at increasing step-economy by withdrawing the intermediate purification of the free azetidine. A one-pot sequence was therefore developed to enable the bis-arylation of azetidines directly from 1, given that both steps of strain-release and Buchwald-Hartwig coupling are performed in the same solvent system. In situ generation of ABB 2 was followed by ring opening with aryl magnesium species, and finally engaged in the coupling reaction under Pd-catalysed conditions described above without purification (Scheme 5). Compounds 7a and 9a were isolated in slightly lower yields than in the twostep procedure. Varying the nature of aryl Grignard reagents led to functionalized scaffolds 10a-f in moderate to good yields after Buchwald-Hartwig C-N coupling with aryl bromides, including substituted phenyl, pyrazine and quinoline moieties.