新型噁唑烷酮类化合物的合成及其抗凝血活性测试

Synthesis and anti-coagulant activities of new oxazolidinone

目的合成一系列新型噁唑烷酮类化合物并考察其抗凝血活性。方法以利奈唑胺为先导化合物,采用Me-too策略,以(R)-N-{[(3-氟-4-羟基苯基)-2-氧代噁唑烷-5-基]甲基}乙酰胺1为起始原料,经过两次亲核取代反应,得到目标化合物,通过凝血时间的比较评价化合物活性。结果合成了6个噁唑烷酮类化合物,其结构经1H-NMR和MS谱确证。结论 6个化合物均有一定的抗凝血活性。

Objective To synthesize a series of oxazolidinone compounds with new structure and study their anticoagu- lant activity.Methods Taking linezolid as lead compound, the Me-too strategy was used and the starting material was （R） -N- { [ （ 3-fluorine-4-hydroxyphenyl ） -2-oxo-oxazolidin-5-yl ] methyl } acetamide 1, underwent two times of nueleophilic substitution reaction, then the target compounds were finally gained. The activities of target compounds were appraised by comparing clotting time.Results Six target compounds were synthesized and their structures were confirmed by I H-NMR and MS spectral methods,respectively.Conclusion The six oxazolidinone compounds all had considerable anti-clotting ac- tivity.