Pd-Catalyzed Picolinamide-Directed C(sp2)–H Sulfonylation of Amino Acids/Peptides with Sodium Sulfinates,The Journal of Organic Chemistry

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Pd-Catalyzed Picolinamide-Directed C(sp2)–H Sulfonylation of Amino Acids/Peptides with Sodium Sulfinates
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2024-06-26 , DOI: 10.1021/acs.joc.4c00988
Raghunath Bag _{1,

2} , Nagendra K Sharma _{1,

2}

Affiliation

This report describes a Pd-catalyzed picolinamide-directed site-selective C(sp²)–H sulfonylation of amino acids and peptides with sodium sulfinates in moderate to good yields. Sulfonylation of levodopa and dopamine drug molecules and late-stage directed peptide sulfonylation are studied for the first time. Broad substrate scope having various functionalities, late-stage drug modifications, and various post synthetic utilities such as chalcogenation, bromination, olefination, and arylation are potential advantages.

中文翻译：

Pd 催化的吡啶甲酰胺定向 C（sp2）–H 氨基磺酰化氨基酸/肽与亚磺酸钠

本报告描述了 Pd 催化的吡啶甲酰胺定向位点选择性 C（sp²）-H 氨基酸和肽与亚磺酸钠的磺酰化反应，产率中等至良好。首次研究了左旋多巴和多巴胺药物分子的磺酰化以及晚期定向肽磺酰化。潜在的优势包括具有各种功能的广泛底物范围、后期药物修饰以及各种合成后实用程序，如硫属化、溴化、烯化和芳基化。

更新日期：2024-06-26

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