Scalable Synthesis of N ‐Acetylated α‐Amino Acid‐Derived Oxazoline Ligands

A scalable cost‐effective synthesis of promising α‐amino acid‐derived oxazoline ligands has been developed. The advantage of the reported procedures is the use of crystallization for the purification of key intermediates and final products. The ligands obtained have recently demonstrated remarkable enantioselectivity in Pd (II) catalyzed C─H activation reactions. Hence, more rational synthetic route presented here will contribute to this rapidly growing field of chemistry.