Summary: Acetamides of theophylline-7-acetic acid (7-TAA) with amino acids were synthesized via a cost effective method directly from theophylline. The synthetic protocols involve: first the synthesis of N-chloroacetyl amino acid methyl ester, and second, its consequent interaction with deprotonated theophylline to give the corresponding acetamide. The described method is characterized with cost effectiveness and good yields.