Utvikling og bruk av selektive oksidative avstengningsringer med flere sulfhydrylgrupper

Utvikling og bruk av selektive oksidative avstengningsringer med flere sulfhydrylgrupper

Research background and challenges

Selective ring closure of multiple sulfhydryl compounds is a key step in the synthesis of sulfur-containing heterocyclic compounds, but the traditional method has the following problems:

  • Multiple sulfhydryl reaction activities are similar, making it difficult to achieve selective control. Many side reactions, complex products, and difficult to isolate and purify. The reaction conditions are harsh and the scope of application is limited. We have successfully developed a new selective oxidative ring-closing technology, which completely solves the above problems and achieves efficient and precise ring-closing reaction.

Technical breakthroughs

  • Innovative oxidation system: The first alkyne amide-based oxidation system is proposed, which significantly improves the selectivity.
  • Unique reaction design: through a variety of different positions of the sulfhydryl substrate, the precise ring closure of multiple sulfhydryl substrates is achieved.

Technical Advantages

  • High selectivity: precise identification of target sites among multiple sulfhydryl substrates to achieve single product generation.
  • High efficiency: the reaction conditions are mild, and the reaction yield is significantly improved.
  • Universality: applicable to the synthesis of various sulfur-containing heterocyclic compounds.

Application Fields

  • Drug synthesis: construction of sulfur-containing heterocyclic drug molecules (f.eks., thiophene, benzothiophene, dithiopyrrolidine, osv.).
  • Functional materials: preparation of sulfur-containing polymer materials (e.g. self-repairing materials, conductive polymers, osv.).
  • Chemical biology: study the formation and function of protein disulfide bonds.

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Xiaoxia Chen

Nytt stoff R&D Tekniker Kjernekompetanse: Måloppdagelse, struktur-aktivitet forhold (SAR) analyse, peptid-legemiddelkonjugater (PDC-er), og utvikling av anti-aldring og metabolske peptider.

Profil: Xiaoxia Chen har ledet den tidlige oppdagelsen og preklinisk forskning for flere metabolske og tumormålrettede peptidmedisiner. Hun er ikke bare dyktig i high-throughput screening av peptidbiblioteker, men også dyktig i å bruke AI-assistert beregningsbiologi for de novo peptidsekvensdesign. For tiden, hun leder et team dedikert til dyptgående forskning og utvikling av neste generasjons multifunksjonelle agonister (for eksempel dobbelt- eller trippelmål-fettreduserende peptider) og svært aktive vevsreparerende peptider.

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