One-pot Synthesis of Chemical Delivery Systems for Gamma-aminobutyric Acid and its Analogues

Abstract

Introduction: A one-pot synthesis route was proposed for the synthesis of chemical delivery systems of bifunctional compounds containing carboxylic- and amino groups, such as gamma-aminobutyric acid and its structural analogues, gabapentin and phenibut. Methods: To obtain targeted compounds, consecutive esterification, amidation, methylation, and reduction were employed in contrast to a more traditional approach that requires isolation and purification of semi-products after each reaction step. Results: A significant (nearly two-fold) increase in yields was observed when target compounds were synthesized using a one-pot approach compared to the conventional one. Conclusion: One-pot approach is a possible and beneficial way for the synthesis of chemical delivery systems for gabapentinoids and other drugs containing carboxylic and amino groups.