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Document Type and Number:
WIPO Patent Application WO/2009/079876
Kind Code:
Disclosed is the 3-acylated shikimic acid or methyl (ethyl) shikimate derivatives. Shikimic acid is a kind of natural product having physiological activity and has effects on thrombus and alleviating brain damage caused by focal cerebral ischemia. However, it cannot be absorbed easily with high polarity, and thus it is important to produce the monoacylated derivatives, improve the polarity, and enhance the fat solubility and the ability of crossing the blood-brain barrier. 3-acylated shikimic acid or methyl (ethyl) shikimate derivatives will be a kind of compounds having unique physiological activity and may be developed into a new class of pharmaceuticals; meanwhile, 3-acylated shikimic acid or methyl (ethyl) shikimate derivatives keep the three chiral centers of the shikimic acid perfectly in structure, and thus they can be useful starting materials and intermediates for synthesizing chiral pharmaceuticals.

TANG, Luhong (No.1800, Lihu AvenueWuxi, Jiangsu 2, 214122, CN)
汤鲁宏 (中国江苏省无锡市蠡湖大道1800号, Jiangsu 2, 214122, CN)
Application Number:
Publication Date:
July 02, 2009
Filing Date:
December 18, 2007
Export Citation:
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JIANGNAN UNIVERSITY (State University Science & Technology Garden, 94 Xinhua Road New District,Wuxi, Jiangsu 8, 214028, CN)
江南大学 (中国江苏省无锡市新区新华路94号江南大学国家大学科技园, Jiangsu 8, 214028, CN)
TANG, Luhong (No.1800, Lihu AvenueWuxi, Jiangsu 2, 214122, CN)
International Classes:
C07C69/013; A61P7/02; C07C62/32; C07C69/75; C07C69/757; C12P7/62
Foreign References:
Other References:
A. NURIA ET AL.: "Regioselective Enzymatic Acylation of Methyl Shikimate. Influence of Acyl Chain Length and Solvent Polarity on Enzyme Specificity", J. ORG. CHEM., vol. 67, no. 14, 2002, pages 4978 - 4981, XP002974845, DOI: doi:10.1021/jo025671p
CHONG ZHAOZHONG ET AL.: "Effects oftriacetylshikimic acid on brain damage and blood rheology after focal cerebral ischemia", CHIN. PHARM. J., vol. 35, no. 8, 2000, pages 520 - 523
WANG NA: "Drug Derivatization by Enzymatic Methods and Preparation of Optically Pure Drug and Polymeric Prodrug", THE PAPER OF DOCTOR'S DEGREE OF ZHEJIANG UNIVERSITY, 2006
Attorney, Agent or Firm:
NANJING TIANHUA PATENT AGENT CO., LTD. (Floor 23, Block A1 World Trade Center Building,No. 67 Shanxi Roa, Nanjing Jiangsu 9, 210009, CN)
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