(S)-(-)-5-Ethynyl-3-(1-methyl-2-pyrroli-dinyl) pyridine Maleate (SIB-1508Y): A Novel Anti-Parkinsonian Agent with Selectivity for Neuronal Nicotinic Acetylcholine …

…, JP Whitten, P Adams, L Chavez-Noriega…

文献索引：Cosford; Bleicher; Herbaut; McCallum; Vernier J.-; Dawson; Whitten; Adams; Chavez-Noriega; Correa; Crona; Mahaffy; Menzaghi; Rao; Reid; Sacaan; Santori; Stauderman; Whelan; et Journal of Medicinal Chemistry, 1996 , vol. 39, # 17 p. 3235 - 3237

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被引用次数: 105

摘要

rolidinone anion followed by decarboxylation and ring closure of the intermediate gave the imine 4. Reduction (NaBH4) and N-methylation under Eschweiler-Clarke conditions13 afforded 5. 14a Palladium-catalyzed crosscoupling15 of 5 with 2-methyl-3-butyn-2-ol provided the 5-alkynyl derivative 6 which underwent base-catalyzed deprotection16 to give 2. 14b Conversion of 2 to 7 was achieved by hydrogenation (H2, Pd-C). 14b In order to ...