Synthesis of Conformationally Restricted Analogs of Baclofen, a Potent GABA_B Receptor Agonist, by the Introduction of a Cyclopropane Ring

概要

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Conformationally restricted analogs of baclofen (2), i.e., 5,6,and their enantiomers ent-5,and ent-6,the conformations of which were restricted by introducing a cyclopropane ring, were designed as potential GABA_B receptor ligands. Reaction of (R)-epichlorohydrin [(R)-7] and (4-chlorophenyl)acetonitrile in the presence of NaNH-2,in benzene/tetrahydrofuran gave chiral cyclopropane derivatives 11 and 12,which were then converted into the target compounds 5 and 6,respectively. Their corresponding enantiomers, ent-5 and ent-6,were also synthesized starting from (S)-epichlorohydring [(S)-7].
社団法人日本薬学会の論文
1999-08-15