New guanidinylation reagents are reported. These reagents consist of N, N', N''-tri-Boc- guanidine (1) and N, N', N''-tri-Cbz-guanidine (2), which allow for the facile conversion of alcohols to substituted guanidines. A series of arginine analogues were synthesized via condensation of a primary or secondary alcohol with the guanidinylation reagents 1 or 2, under Mitsunobu conditions, 1 to produce protected alkylated guanidines. In addition, an ...
