ET_A受体拮抗剂杨梅酸A的半合成研究

Study of the Partial Synthesis of Myriceric Acid A of Endothelin A Receptor Antagonist

合成了潜在的特定ETA受体拮抗剂杨梅酸A。合成方法是通过廉价易得的齐墩果酸为原料,通过3-OH Dess-Martin(DMP)氧化、臭氧化、液氨还原等11步反应,得到杨梅酸A,中间体及目标产物的结构通过1H NMR、13C NMR进行了表征。

a potent and specific myriceric acid A of endothelin A receptor antagonist was synthesised by using abundant cheap oleanolic acid through 11 reaction steps of Dess-Martin oxidation, ozone oxide process, Birch reduction etc. in this paper. A highly efficient and practical synthesis was developed. The structures of intermediate product and TM are confirmed by ^1H NMR,^13C NMR.