Gregg Brian T, Tymoshenko Dmytro O, Razzano Dana A, Johnson Matthew R
Albany Molecular Research, Inc., 21 Corporate Circle, Albany, New York, 12212, USA.
J Comb Chem. 2007 May-Jun;9(3):507-12. doi: 10.1021/cc0700039. Epub 2007 Apr 18.
The pyrazolo[1,5-a]pyrimidine class of compounds has been identified as a privileged structure for library synthesis on the basis of several key characteristics of the core molecule. A chemical set in excess of 400 compounds was synthesized to give 3,6,7-substituted pyrazolo[1,5-a]pyrimidinecarboxamides 9. To facilitate the rapid preparation of this library, a preparative strategy included the synthesis of activated p-nitrophenyl esters, followed by subsequent scavenging of the p-nitrophenol leaving group. Excess reagents were also removed using scavenging reagents that were found to be compatible with the synthetic methodology and that afforded target compounds in acceptable purity and yields.
基于核心分子的几个关键特征，吡唑并[1,5 - a]嘧啶类化合物已被确定为用于文库合成的优势结构。合成了一组超过400种化合物的化学集，以得到3,6,7 - 取代的吡唑并[1,5 - a]嘧啶甲酰胺9。为了便于快速制备该文库，一种制备策略包括合成活性对硝基苯酯，随后清除对硝基苯酚离去基团。还使用了与合成方法兼容且能以可接受的纯度和产率提供目标化合物的清除剂去除过量试剂。
