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.

Keywords: Chemical delivery systems, One-pot synthesis, Gamma-amino butyric acid, Gabapentin, Phenibut, Semi-products.
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