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The Synthesis and Structural Modification of Novel Natural Product-Selaginellin L

Author: LiuRui
Tutor: TanGuiShan
School: Central South University
Course: Medicinal Chemistry
Keywords: mGluR5 antagonists Selaginellin L ND-Selaginellin MPEPa
CLC: R284.1
Type: Master's thesis
Year: 2011
Downloads: 56
Quote: 1
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Abstract


Currently , the screening found mGluR5 antagonist synthetic chemical entities are based on computer-aided drug design compound libraries . So far, no mGluR5 antagonist derived from a natural product literature reports. 2007 Lanzhou University Lister first isolated from Selaginella sinensis to new carbon skeleton Selaginellin the alkyne phenolic chemical structure . Subsequently, the experimental group success from Selaginella genus 12 to get Selaginellin series of compounds . Subject early stage of Selaginellin biologically active research and literature analysis , we may speculate Selaginellin L is an excellent natural mGluR5 antagonist . The topic for the first time as a natural product Selaginellin L lead compounds , the to design synthetic the ND-Selaginellin class goal the compound and MPEPa class target compounds . By bromination, Suzuki in Sonogashira diazotization reaction successfully synthesized compound , ND - Selaginellin class compounds 13 and 10 , MPEPa compounds . The structures were confirmed by 1HNMR, 13CNMR modern spectroscopic techniques of related compounds . In addition , the subject , the route of synthesis of the related compounds exploration, where the design of the three target compounds 9 ( 4,4 ??' - dimethoxy -5 - (( 4 - methoxyphenyl) ethynyl ) -2 - methyldibenzo ) in the synthetic route, and successfully opened route 3 ; designed two of the target compound 17 ( 4 ' , 6 - dimethoxy-3 - ((4 - methoxyphenyl) ethynyl ) - 2 - methyl diphenyl ) synthesis route , the two routes to get through successfully . In addition, some important chemical reactions in the field of medicine and chemical , such as bromo , Suzuki, in Sonogashira such as a large number of exploration to find the better method of preparation . The same time, the substrate salt of fluorine boron as the Suzuki reaction , we also found a novel extension of the carbon chain .

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CLC: > Medicine, health > Chinese Medicine > Of Pharmacy > Traditional Chinese medicine chemical > Chemical analysis and identification
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