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Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
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Author Spotlight: An Efficient Methodology to Confidently Differentiate and Characterize Fentanyl Analogs
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Total Synthesis of Fexuprazan.

Tae Lyn Kim1, Jinyeong Jeon1, Cheol-Hong Cheon1

  • 1Department of Chemistry, Korea University, 145 Anam-ro, Seongbuk-gu, Seoul 02841, Republic of Korea.

Organic Letters
|March 26, 2026
PubMed
Summary

A new, practical synthesis for fexuprazan was developed using Strecker or reductive amination pathways. This efficient route yields gram-scale fexuprazan with simple purification, highlighting its industrial applicability.

Area of Science:

  • Organic Chemistry
  • Medicinal Chemistry
  • Process Chemistry

Background:

  • Fexuprazan is a potassium-competitive acid blocker.
  • Developing efficient synthetic routes is crucial for pharmaceutical production.

Purpose of the Study:

  • To develop a novel and practical synthetic route to fexuprazan.
  • To achieve gram-scale synthesis with high efficiency and simple purification.

Main Methods:

  • Two complementary approaches for synthesizing a key N-sulfonyl α-amino ester intermediate.
  • Utilized Strecker reaction or reductive amination for intermediate synthesis.
  • Employed Michael addition, intramolecular Wittig reaction, oxidation, decarboxylation, and functional group conversion to obtain fexuprazan.

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Main Results:

  • Successfully synthesized fexuprazan via a multi-step sequence.
  • Demonstrated efficient access to key intermediates.
  • Achieved gram-scale production with intermediates and final product isolated by simple recrystallization.

Conclusions:

  • The developed synthetic route is novel, practical, and efficient for fexuprazan production.
  • The method's simplicity and scalability underscore its potential for industrial application.
  • Highlights the feasibility of producing fexuprazan on a gram scale with high purity.