Catalytic Enantioselective Intramolecular C(sp³)−H Amination of 2‐Azidoacetamides

An enantioselective ring-closing C(sp3 )-H amination of 2-azidoacetamides is catalyzed by a chiral-at-metal ruthenium complex and provides chiral imidazolidin-4-ones in 31-95 % yield, with enantioselectivities of up to 95 % ee, and at catalyst loadings down to 0.1 mol % (turnover number (TON)=740). To our knowledge, this is the first example of a highly enantioselective C(sp3 )-H amination with aliphatic azides. Mechanistic experiments reveal...