Saturated N-and O-heterocycles are widespread motifs in natural products and marketed drugs, as well as valuable building blocks in medicinal chemistry. Recently, there has been an increased drive to include saturated heterocycles in screening libraries, as well as an empirically observed link between sp -rich structures and lower attrition rate in drug discovery programs. Small saturated heterocycles are advantageous starting points in fragment-based drug discovery due to their low molecular weight, propensity for H-bonding and potential for 3D growth-vectors along the C(sp 3 )-H bonds. The ability to expediently access any defined substitution pattern would hence be highly desired to elaborate a lead or fragment hit.