Vasquez Thomas E, Nixey Thomas, Chenera Balan, Gore Vijay, Bartberger Michael D, Sun Yaxiong, Hulme Christopher
Medicinal Chemistry Technologies, Chemistry Research and Development, AMGEN, One AMGEN Center Drive, Thousand Oaks, CA 91320, USA.
Mol Divers. 2003;7(2-4):161-4. doi: 10.1023/b:modi.0000006917.06401.48.
The novel solution-phase synthesis of an array of biologically relevant pyrazoloquinazolinones in a simple microwave driven one pot procedure is revelaed. Transformations are carried out in good to excellent yield by condensation of alpha-cyano-ketones and 2-hydrazino-benzoic acids. Subsequent microwave irradiation affords pyrazoloquinazolinones with six points of potential diversification. The protocol described represents a very attractive solution phase procedure for the rapid generation of arrays of such functionalized cores, further demonstrating the growing importance of economic and enabling complexity generating chemistries in the lead discovery arena.
本文揭示了一种在简单的微波驱动单锅法中，新型的、用于合成一系列具有生物学相关性的吡唑并喹唑啉酮的溶液相合成方法。通过α-氰基酮与2-肼基苯甲酸的缩合反应，反应转化率良好至优异。随后的微波辐射得到具有六个潜在多样化位点的吡唑并喹唑啉酮。所描述的方案代表了一种非常有吸引力的溶液相方法，用于快速生成此类功能化核心的阵列，进一步证明了经济且能够产生复杂性的化学方法在先导化合物发现领域的重要性日益增加。
