アリールピペラジン合成研究の回顧と展望

抄録

Arylpiperazines are important core structure for CNS drug substances and hence, many synthetic endeavors have been made for efficient entry into the requisite molecular alignment including Buchwald/Hartwig amination, Wynberg amination and other catalytic methods, whereby a variety of new options have been developed and to be noted for medicinal chemistry research. In this presentation some utility of Wynberg amination is emphasized where Buchwald-Hartwig amination reaction failed. For the conversion of poly-halogenated benzenes, Wynberg amination is quite effective starting with readily available anisol derivatives. Furthermore, interesting fragmentation-ring closure was observed to afford acridine skeleton via presumed benzyne intermediacy as shown below.