细胞周期蛋白依赖性激酶抑制剂(CDKs)中间体的设计与合成

Design and Synthesis of Intermediate of the Cell Cycle Protein Kinase Inhibitors(CDKs)

简述了细胞周期蛋白依赖性激酶CDK4抑制剂及其抑制剂的相关概念,详细介绍了细胞周期蛋白激酶的研究进展,重点研究了中间体2-溴-1-(4-吗啉苯基)乙酮的路线选择与合成。4-氟苯乙酮为起始原料,经过溴代反应合成2-溴-1-(4-吗啉苯基)乙酮。依据文献报道,比较不同的合成路线,最终选择先溴代再脱溴的方法合成目标化合物。

The cyclin-dependent kinase （CDK4） inhibitors were introduced, research progress in cyclin kinase was summed up. Synthesis routes of intermediate 2-bromo-l-（4-morpholinophenyl）-l-ethanone was studied. 4-Fluoroacetophenone was used as raw material to synthesize 2-bromo-l-（4-morpholinophenyl）-l-ethanone by bromination reaction.Based on literatures,different synthesis routes were compared.The bromination-debromination synthesis route was finally chosen to synthesize target compound.