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多肽药物吸收促进剂8-水杨酰胺基辛酸的合成

Synthesis of Heparin Delivery Agent N-(Salicyloyl)-8-aminocaprylic Acid

  • 摘要: 目的:合成8-水杨酰氨基辛酸作为肝素等多肽药物口服给药的促进剂。方法:环辛酮通过成肟、重排、水解3步反应制得8-氨基辛酸,然后与水杨酸低聚酯进行酰化反应,得8-水杨酰胺基辛酸。结果和讨论:目的物结构经IR、^1HNMR、^13CNMR和MS得到确证,对肝素等多肽药物口服给药的促进活性正在进一步研究之中。

     

    Abstract: AIM:To synthesize N-(salicyloyl)-8-am inocaprylic acid as the delivery agent of oral heparin METHOD:Object compone n t,N-(salicyloyl)-8-aminocaprylic acid,and its sodium salt were synthes ized beg inning with cyclooctanone by oximation,rearrangement and

     

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