Applications of N-BOC-diamines for the solution phase synthesis of ketopiperazine libraries utilizing a Ugi/De-BOC/Cyclization (UDC) strategy
作者:Christopher Hulme、John Peng、Bonnie Louridas、Paul Menard、Paul Krolikowski、N.Vasant Kumar
DOI:10.1016/s0040-4039(98)01770-5
日期:1998.10
This communication reveals a novel application of the ‘so-called’ convertible isonitrile for the solution phase generation of ketopiperazine libraries. Use of mono N-BOC diamines in the Ugi multi-component reaction (MCR), followed by BOC removal and base treatment (a ‘3 step, 1-pot procedure’) affords ketopiperazines in good yield. The generality of this procedure was further explored revealing novel
这种交流揭示了“所谓的”可转换异腈在酮戊哌嗪文库的溶液相生成中的新应用。在Ugi多组分反应(MCR)中使用单N-BOC二胺,然后进行BOC去除和碱处理(“ 3步1锅法”),得到的酮哌嗪具有良好的收率。进一步探讨了该方法的一般性,揭示了分别制备二氢喹喔啉酮和1,4-苯并二氮杂novel的新途径。