One-Step Synthesis of Benorilate Guided by Green Chemistry Principles and in vivo Dynamic Evaluation
The current synthesis of benorilate typically involves the Schotten-Baumann esterification,which generates harmful gases HCl and SO2 from the reagent SOCl2,posing environmental concerns. Moreover,the process entails multiple steps. In this study,we have optimized a one-step method using EDCI/4-DMAP esterification for the synthesis of benorilate. The product's structure and purity were characterized through melting point determination,NMR,and HPLC-MS analysis,followed by in vivo dynamic evaluation in rats based on plasma and bile samples. This evaluation confirmed the principles of drug design. The improved method not only enhances efficiency but also significantly improves experimental safety.
BenorilateOne-step synthesisEDCIIn vivo analysisCombination principles
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