Direct Aminoalkylation of Arenes and Hetarenes via Ni-Catalyzed Negishi Cross-Coupling Reactions
作者:Laurin Melzig、Andrey Gavryushin、Paul Knochel
DOI:10.1021/ol702499h
日期:2007.12.1
room-temperature Ni-catalyzed cross-coupling of aminoalkylzinc halides, readily available from the corresponding aminoalkyl chlorides via Grignard reagents, with aryl and hetaryl electrophiles, allows a convenient one-step preparation of aminoalkyl (het)arenes, bearing a basic tertiary nitrogen in the side chain, including piperidine and tropane derivatives. Such aminoalkylarene scaffolds are widely present in
氨基烷基锌卤化物的直接室温Ni催化交叉偶联很容易从相应的氨基烷基氯化物通过Grignard试剂与芳基和杂芳基亲电试剂获得,可以方便地一步制备带有碱性叔胺的氨基烷基(杂)芳烃侧链中的氮包括哌啶和托烷衍生物。这种氨基烷基亚芳基支架广泛存在于各种生物活性分子中。