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Citation: Bingliang Li, Yuying Han, Dianyang Li, Dandan Liu, Wenbin Shang. One-Step Synthesis of Benorilate Guided by Green Chemistry Principles and in vivo Dynamic Evaluation[J]. University Chemistry, ;2024, 39(6): 342-349. doi: 10.3866/PKU.DXHX202311070 shu

One-Step Synthesis of Benorilate Guided by Green Chemistry Principles and in vivo Dynamic Evaluation

1.
School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, China;
2.
College of Modern Biomedical Industry, Kunming Medical University, Kunming 650500, China

Received Date: 21 November 2023
Revised Date: 5 January 2024

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.
- Benorilate,
- One-step synthesis,
- EDCI,
- In vivo analysis,
- Combination principles
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