Catalytic amination of 2-substituted pyridines with hydrazine derivatives

被引:86
作者
Arterburn, JB [1 ]
Rao, KV [1 ]
Ramdas, R [1 ]
Dible, BR [1 ]
机构
[1] New Mexico State Univ, Dept Chem & Biochem, Las Cruces, NM 88003 USA
关键词
D O I
10.1021/ol015731y
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[GRAPHICS] 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.
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页码:1351 / 1354
页数:4
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