烟台大学学报（自然科学与工程版）
煙檯大學學報（自然科學與工程版）
연태대학학보（자연과학여공정판）
JOURNAL OF YANTAI UNIVERSITY（NATURAL SCIENCE AND ENGINEERING EDITION）
2015年
1期
30-33
,共4页
刘兴东%蔡艺%张晰月%杨帆%朱伟伟%白国静%孟庆国
劉興東%蔡藝%張晰月%楊帆%硃偉偉%白國靜%孟慶國
류흥동%채예%장석월%양범%주위위%백국정%맹경국
黄芩苷%酯%衍生物%合成
黃芩苷%酯%衍生物%閤成
황금감%지%연생물%합성
baicalin%ester%derivative%synthesis
基于前药设计原理,设计合成了6个黄芩苷酯类衍生物.黄芩苷与甲烷磺酸甲酯、甲烷磺酸乙酯反应,得到目标化合物1和2.黄芩苷与乙酸酐反应,得到化合物3,3分别与甲烷磺酸甲酯、甲烷磺酸乙酯和甲烷磺酸异丙酯反应,得到目标化合物4、5和6.化合物结构均经ESI-MS和1 H NMR确证.化合物4、5和6易溶于乙酸乙酯,具有较好的脂溶性.
基于前藥設計原理,設計閤成瞭6箇黃芩苷酯類衍生物.黃芩苷與甲烷磺痠甲酯、甲烷磺痠乙酯反應,得到目標化閤物1和2.黃芩苷與乙痠酐反應,得到化閤物3,3分彆與甲烷磺痠甲酯、甲烷磺痠乙酯和甲烷磺痠異丙酯反應,得到目標化閤物4、5和6.化閤物結構均經ESI-MS和1 H NMR確證.化閤物4、5和6易溶于乙痠乙酯,具有較好的脂溶性.
기우전약설계원리,설계합성료6개황금감지류연생물.황금감여갑완광산갑지、갑완광산을지반응,득도목표화합물1화2.황금감여을산항반응,득도화합물3,3분별여갑완광산갑지、갑완광산을지화갑완광산이병지반응,득도목표화합물4、5화6.화합물결구균경ESI-MS화1 H NMR학증.화합물4、5화6역용우을산을지,구유교호적지용성.
Based on the principle of pro-drug design, six ester-type derivatives derived from baicalin have been de-signed and synthesized. Compound 1 and compound 2 have been obtained from baicalin by ethanoylation. Com-pounds 4 , compound 5 and compound 6 have been prepared from compound 3 by esterification with methyl mesy-late, ethyl mesylate and i-propyl mesylate, respectively. Their structures are elucidated by means of ESI-MS and 1 H NMR. Compounds 4, compound 5 and compound 6 can dissolve in ethyl acetate with good liposolubility.
