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Isothiocyanate intermediates facilitate divergent synthesis of N-heterocycles for DNA-encoded libraries.
Wang, Huihong; Chen, Teng; Fan, Xiaohong; Li, Yangfeng; Fang, Wei; Zhang, Gong; Li, Yizhou.
Afiliación
  • Wang H; Pharmaceutical Department, Chongqing University Three Gorges Hospital, Chongqing University, 404100 Chongqing, P. R. China. delight9924@163.com.
  • Chen T; Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, China. yizhouli@cqu.edu.cn.
  • Fan X; Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, China. yizhouli@cqu.edu.cn.
  • Li Y; Pharmaceutical Department, Chongqing University Three Gorges Hospital, Chongqing University, 404100 Chongqing, P. R. China. delight9924@163.com.
  • Fang W; Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, China. yizhouli@cqu.edu.cn.
  • Zhang G; Pharmaceutical Department, Chongqing University Three Gorges Hospital, Chongqing University, 404100 Chongqing, P. R. China. delight9924@163.com.
  • Li Y; Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, China. yizhouli@cqu.edu.cn.
Chem Commun (Camb) ; 60(59): 7638-7641, 2024 Jul 18.
Article en En | MEDLINE | ID: mdl-38963238
ABSTRACT
The versatile reactivity of isothiocyanate intermediates enabled the diversity-oriented synthesis (DOS) of N-heterocycles in a DNA-compatible manner. We first reported a mild in situ conversion of DNA-conjugated amines to isothiocyanates. Subsequently, a set of diverse transformations was successfully developed to construct 2-thioxo-quinazolinones, 1,2,4-thiadiazoles, and 2-imino thiazolines. Finally, the feasibility of these approaches in constructing DELs was further demonstrated through enzymatic ligation and mock pool preparation. This study demonstrated the advantages of combining in situ conversion strategies with DOS, which effectively broadened the chemical and structural diversity of DELs.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: ADN / Isotiocianatos / Compuestos Heterocíclicos Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2024 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: ADN / Isotiocianatos / Compuestos Heterocíclicos Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2024 Tipo del documento: Article Pais de publicación: Reino Unido