Stereoselective syntheses of highly functionalized bicyclo[3.1.0]hexanes: a general methodology for the synthesis of potent and selective mGluR2/3 agonists.
摘要：
[Chemical reaction: See text] A Et3Al mediated intramolecular epoxide opening, cyclopropanation reaction is described. The transformation provided highly functionalized bicyclo[3.1.0]hexane systems in high efficiency and with perfect H or F endo selectivity. Application of this reaction to the synthesis of mGluR2/3 agonist 1 (43% overall yield) and a few intermediates suitable for the synthesis of other bicyclo[3.1.0]hexane mGluR2/3 agonists is discussed.
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关键词：
METABOTROPIC GLUTAMATE RECEPTORS (+)-2-AMINOBICYCLO<3.1.0>HEXANE-2 6-DICARBOXYLIC ACID LY354740 PHARMACOLOGICAL CHARACTERIZATION 1-FLUOROCYCLOPROPANE-1-CARBOXYLATE DERIVATIVES ASYMMETRIC-SYNTHESIS MOLECULAR DIVERSITY BRAIN-FUNCTION REARRANGEMENT ROUTE RATS
DOI：
10.1021/jo0511187
被引量：
年份：
2005
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