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-aminocap rylic Acid

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、1 HNMR、1 3 CNMR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。

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 hydrolysis to obtain 8 -aminocaprylic acid And then 8-aminocaprylic acid was esterified by ologosal icylate to obtain the product RESULT:The structures of the object components were identified by IR, 1 HNMR, 13 CNMR and M S spectr a,and the delivery activity of oral heparin and other drugs is on researching