Arterburn J B, Rao K V, Ramdas R, Dible B R
Department of Chemistry and Biochemistry, MSC 3C, New Mexico State University, P.O. Box 30001, Las Cruces, New Mexico 88003, USA.
Org Lett. 2001 May 3;3(9):1351-4. doi: 10.1021/ol015731y.
[reaction in text] Protected pyridylhydrazine derivatives were prepared in a one-step palladium-catalyzed amination reaction using chelating phosphine ligands. 2-Pyridyl chlorides, bromides, and triflates were effective electrophiles in these reactions. Di-tert-butyl hydrazodiformate was an excellent hydrazine substrate, and the resulting products were deprotected under mild conditions. Catalytic amination provides a direct route to protected bifunctional hydrazinopyridine linkers that are suitable for metal-bioconjugate syntheses.
[文本中的反应] 使用螯合膦配体，通过一步钯催化胺化反应制备了受保护的吡啶基肼衍生物。2-吡啶基氯化物、溴化物和三氟甲磺酸盐在这些反应中是有效的亲电试剂。二叔丁基偶氮二甲酸酯是一种优良的肼底物，所得产物在温和条件下脱保护。催化胺化提供了一条直接合成受保护的双功能肼基吡啶连接体的途径，该连接体适用于金属-生物共轭物的合成。
