薯蓣皂甙元丁二酸单酯氨基酸盐的合成及其动物实验——薯蓣皂甙元衍生物的研究I

SYNTHESIS OF DIOSGENIN SUCCINIC MONO-ESTER DERIVATIVES AND RESEARCH OF APLLICATION

以薯蓣皂甙元丁二酸单酯为原料 ,经过与氨基酸缩合 ,合成了 5个新化合物 ,4 L (N 丁二酸 2 基 )胺基 4 氧代丁酸薯蓣皂甙元酯二钠盐 (1) ,4 (N 乙酸 2 基 )胺基 4 氧代丁酸薯蓣皂甙元酯钠盐(2 ) ,4 L (N (5 胍基 )戊酸 2 基 )胺基 4 氧代丁酸薯蓣皂甙元酯醋酸盐 (3) ,4 (N (3 咪唑 4 基 )丙酸 2 基 )胺基 4 氧代丁酸薯蓣皂甙元酯醋酸盐 (4) ,4 (N 戊二酸 2 基 )胺基 4 氧代丁酸薯蓣皂甙元酯二钠盐(5 ) ,并对其进行了结构鉴定 ,同时发现这 5个化合物对大鼠都具有抗心肌梗死活性。

Five new compounds were synthesized from diosgenin succinic mono-ester via condensation with Amino acids,their structures were determined by 1HNMR?MS and IR as disodium diosgeninyl 4-L-(N-succinic acid-2-yl)amino-4-oxo butyrate(1),sodium diosgeninyl 4-(N-acetic acid-2-yl)amino-4-oxo butyrate(2),diosgeninyl 4- L-(N-(5-guanidino)pentanoic acid-2-yl)amino-4-oxo butyrate acetate(3),diosgeninyl 4-(N-3-(4-imidazolyl)propionic acid-2-yl)amino-4-oxo butyrate acetate(4),disodium diosgeninyl 4-(N-glutaric acid-2-yl)amino-4-oxo butyrate(5).All of these compounds show anti-infarction activity on rat.