Tetrahedron letters

Synthesis of conformationally constrained spirodihydrofuropyridine analogues of epibatidine

H Abe, Y Arai, S Aoyagi, C Kibayashi

文献索引：Abe, Hideki; Arai, Yumiko; Aoyagi, Sakae; Kibayashi, Chihiro Tetrahedron Letters, 2003 , vol. 44, # 14 p. 2971 - 2973

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被引用次数: 14

摘要

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.