Ontwikkeling en toepassing van selektiewe oksidatiewe afsluitringe met veelvuldige sulfhidrielgroepe

Ontwikkeling en toepassing van selektiewe oksidatiewe afsluitringe met veelvuldige sulfhidrielgroepe

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 (bv., thiophene, benzothiophene, dithiopyrrolidine, ens.).
  • Functional materials: preparation of sulfur-containing polymer materials (e.g. self-repairing materials, conductive polymers, ens.).
  • Chemical biology: study the formation and function of protein disulfide bonds.

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Xiaoxia Chen

Nuwe dwelm R&D Tegnikus Kernkundigheid: Teiken ontdekking, struktuur-aktiwiteit verhouding (SAR) ontleding, peptied-geneesmiddel konjugate (PDC's), en die ontwikkeling van anti-veroudering en metaboliese peptiede.

Profiel: Xiaoxia Chen het die vroeë ontdekking en prekliniese navorsing gelei vir verskeie metaboliese en tumor-gerigte peptiedmiddels. Sy is nie net vaardig in hoë-deurset sifting van peptied biblioteke nie, maar ook vaardig in die gebruik van KI-gesteunde rekenaarbiologie vir de novo peptied volgorde ontwerp. Tans, sy lei 'n span wat toegewy is aan die in-diepte navorsing en ontwikkeling van volgende generasie multifunksionele agoniste (soos dubbel- of drievoudige teiken vetverminderende peptiede) en hoogs aktiewe weefselherstelpeptiede.

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