Synthesis of cyclic and acyclic Nα-methyl-Nω-alkyl-l-arginine analogues

A series of Nα-methyl-alkyl-l-arginine (Arg) analogues have been synthesized from inexpensive, commercially available starting materials. These analogues, once incorporated into pharmaceutically relevant peptides, are expected to increase binding affinity, receptor selectivity, lipophilicity, and stability as demonstrated with analogues of similar design and structure.