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Synthesis of conformationally constrained spirodihydrofuropyridine analogues of epibatidine

โœ Scribed by Hideki Abe; Yumiko Arai; Sakae Aoyagi; Chihiro Kibayashi

Publisher
Elsevier Science
Year
2003
Tongue
French
Weight
99 KB
Volume
44
Category
Article
ISSN
0040-4039

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โœฆ Synopsis

Conformationally constrained spirofuropyridine analogues of epibatidine, syn-2 and anti-2, in which the 7-azabicyclo[2.2.1]heptane system and the 2-chloropyridine ring are held rigidly with the shorter and longer N-N distances, respectively, were synthesized from N-Boc-7-azabicyclo[2.2.1]heptan-2-one. The preliminary binding studies suggested that syn-2 has stronger binding affinity for nAChRs than anti-2.

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