A one-pot photocleavage ring-opening/reductive amination procedure was developed to access products 5-8 (up to 64% yield over two steps) in a single operation. Leveraging this strategy, it was possible to prepare the highly selective dopamine D3 receptor ligands 7 (BP-897) and 8 in 64% and 71% yield, respectively (Figure , middle). Finally, an optically active 5-oxaproline analog 52 was exposed to the reaction conditions (Figure , low). It is pertinent to note that N-O bond cleavage of this motif was a key step in Vasella's total synthesis of Nojirimycin. This strategy enabled the unnatural amino-acid aldehyde 9 to be formed smoothly in 71% yield. Reductive amination with n-propylamine generated the chiral 1,3-diamine 10 in good yield (76%). It was also possible to access morpholine 11 in good yield (69% after 2 steps) this one-pot protocol.