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过去很大的努力在致力于发现一类在医疗上有用的PG类似物,它们仅具有天然PG各种有效的生物活性中的一种功效,但成绩有限。在此通讯中,我们所描述合成一些海因型PG类似物,它们都是非常有效的血小板聚集抑制剂,此外也具有一定的选择性。如图所示,氨基二酯在室温和缓地和乙烯基酮反应,所得的Mannich碱经二步反应转变为海因酸酯(2)和海因化物(3),总收率很好。在100℃加热此混合物完全转变为(3)后,室温用碱的水溶液水解除去酯基而得两个外消旋非对映立体异构物羧酸(4)。两个异构物可以用薄层层析区分、高压液相层析分离。它们的′HNMR表现出明显的差异,极性小
Much effort in the past was devoted to the discovery of a class of medically useful PG analogues that have only one of a variety of potent biological activities of natural PG with limited success. In this communication, we describe the synthesis of some of the HIN-type PG analogs, which are very potent inhibitors of platelet aggregation and have some selectivity. As shown, the aminodialylester reacted slowly with vinyl ketone at room temperature and the resulting Mannich base was converted to the hydantoin (2) and the hydantoin (3) by a two step reaction with good overall yields. After completely heating the mixture to 100 ° C (3), hydrolysis of the ester group with an aqueous base at room temperature gives the two racemic diastereomeric carboxylic acids (4). The two isomers can be separated by thin layer chromatography and separated by high pressure liquid chromatography. Their ’HNMR showed a clear difference, the polarity is small