Copper-Mediated Three-Component Reaction for the Synthesis of N-Sulfonylamidine on DNA DOI
Taehyun Kwon, Yeonhee Lee, Kyungjin Cho

и другие.

Organic Letters, Год журнала: 2025, Номер unknown

Опубликована: Апрель 11, 2025

DNA-encoded library (DEL) technology is a transformative tool for identifying bioactive compounds in pharmaceutical research. This study presents an optimized copper-mediated reaction to synthesize N-sulfonylamidine derivatives from DNA-conjugated alkynes and sulfonyl azides under mild conditions. Amines serve as nucleophiles, enabling selective functionalization conditions while preserving DNA integrity. Through systematic refinement of substrate evaluation, the approach demonstrated high tolerance diverse functional groups, significantly expanding DEL-accessible chemical space. The developed DNA-compatible method underscores role DELs enhancing drug discovery by facilitating introduction novel pharmacophores into compound libraries.

Язык: Английский

Copper-Mediated Three-Component Reaction for the Synthesis of N-Sulfonylamidine on DNA DOI
Taehyun Kwon, Yeonhee Lee, Kyungjin Cho

и другие.

Organic Letters, Год журнала: 2025, Номер unknown

Опубликована: Апрель 11, 2025

DNA-encoded library (DEL) technology is a transformative tool for identifying bioactive compounds in pharmaceutical research. This study presents an optimized copper-mediated reaction to synthesize N-sulfonylamidine derivatives from DNA-conjugated alkynes and sulfonyl azides under mild conditions. Amines serve as nucleophiles, enabling selective functionalization conditions while preserving DNA integrity. Through systematic refinement of substrate evaluation, the approach demonstrated high tolerance diverse functional groups, significantly expanding DEL-accessible chemical space. The developed DNA-compatible method underscores role DELs enhancing drug discovery by facilitating introduction novel pharmacophores into compound libraries.

Язык: Английский

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