PMID: 10863794Jun 23, 2000Paper

Synthesis of 5-(4-alkoxy-[1,2,5]thiadiazol-3-yl)-3-methyl-1,2,3,4-tetrahydropyrimidi ne oxalate salts and their evaluation as muscarinic receptor agonists

Archiv der Pharmazie
J G ParkM H Jung


The synthesis and biological testing of 5-(4-alkoxy-[1,2,5]thiadiazol-3-yl)-3-methyl-1,2,3,4-tetrahydro pyrimidine oxalate salts 8 as muscarinic receptor agonists are described. The key intermediate 4 was obtained by modified Strecker reaction and cyclization of starting material 1. Subsequent alkoxy substitution, quaternization, and reduction afforded 7. For the sake of purity and stability of the final products 8, the 3-methyl-1,2,3,4-tetrahydropyrimidines were obtained as oxalic acid salts. All final compounds were examined in vitro for their binding affinities to the cloned human muscarinic receptor by the [3H]-NMS binding assay.


Jan 1, 1981·The British Journal of Psychiatry : the Journal of Mental Science·J E ChristieA I Glen
Apr 20, 1994·Biochemical Pharmacology·R M Nitsch, J H Growdon
Feb 16, 1993·European Journal of Pharmacology·R L HudkinsD L DeHaven-Hudkins
Feb 13, 1999·Journal of Medicinal Chemistry·C E Augelli-SzafranA J Thomas

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