Substituent-dependent negative hyperconjugation in 2-aryl-1,3-N,N-heterocycles. Fine-tuned anomeric effect?

The epimerization reactions of conformationally inflexible 2-aryl-1,3-N,N-heterocycles were used as model systems to study the role of the nitrogen lone pair-C2 associated antibonding orbital hyperconjugative interactions in the experimentally observed substituent-dependent generalized anomeric effe...

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Elmentve itt :
Bibliográfiai részletek
Szerzők: Hetényi Anasztázia
Martinek Tamás A.
Lázár László
Zalán Zita
Fülöp Ferenc
Dokumentumtípus: Cikk
Megjelent: American Chemical Society 2003
Sorozat:JOURNAL OF ORGANIC CHEMISTRY 68 No. 14
doi:10.1021/jo034417

mtmt:1013527
Online Access:http://publicatio.bibl.u-szeged.hu/7564
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520 3 |a The epimerization reactions of conformationally inflexible 2-aryl-1,3-N,N-heterocycles were used as model systems to study the role of the nitrogen lone pair-C2 associated antibonding orbital hyperconjugative interactions in the experimentally observed substituent-dependent generalized anomeric effect. The measured reaction free enthalpies were found to correlate well with the sum of the hyperconjugative stabilization energies of all the vicinal donor-acceptor orbital overlaps around C2, obtained from ab initio NBO analysis, and both quantities correlated linearly with the Hammett-Brown substituent constant. The individual stereoelectronic interactions (n(N)-sigma*(C2-N), n(N)-sigma*(C2-Ar), n(N-sigma)*(C2-H)) were also observed to exhibit a substituent dependence, despite their distance from the 2-aryl substituent and their nonperiplanar arrangement. The higher the electron-withdrawing effect of the 2-aryl substituent, the larger was the stabilization for n(N)-sigma*(C2-Ar), while the overlaps n(N)-sigma*(C2-N) and n(N)-sigma*(C2-H) changed in the opposite sense. The different polarization of the acceptor sigma* orbitals, caused by the 2-aryl substituent, accounted for the observed propagation of the substituent effect. These results promote a detailed explanation of the useful tautomeric behavior of the 2-aryl-1,3-X,N-heterocycles, and reveal the nature of the connection between the anomeric effect and the Hammett-type linear free energy relationship. 
700 0 1 |a Martinek Tamás A.  |e aut 
700 0 1 |a Lázár László  |e aut 
700 0 1 |a Zalán Zita  |e aut 
700 0 1 |a Fülöp Ferenc  |e aut 
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