ChemInform Abstract: Tetrahydropyridyloxadiazoles: Semirigid Muscarinic Ligands.
Abstract
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ChemInform Abstract
Arecoline (Ia) and 6-methylarecoline (Ib) react with the amidoximes (II) to give the oxadiazoles (III). Conversion of (I) to the N-protected derivatives (V) followed by coupling with (IIa) or (IIc) and subsequent deprotection yields the NH analogues (VI). Similarly, (IX) is synthesized as shown in the reaction scheme. The derivatives (VIa) and (IX) are the most potent muscarinic antagonists among the compounds prepared.