Theoretical Evidence of Pyramidalized Bicyclic Serine Enolates in Highly Diastereoselective Alkylations
- Aydillo, C. 1
- Jiménez-Osés, G. 1
- Busto, J.H. 1
- Peregrina, J.M. 1
- Zurbano, M.M. 1
- Avenoza, A. 1
-
1
Universidad de La Rioja
info
ISSN: 0947-6539
Año de publicación: 2007
Volumen: 13
Número: 17
Páginas: 4840-4848
Tipo: Artículo
Otras publicaciones en: Chemistry - A European Journal
Resumen
A new chiral serine equivalent and its enantiomer have been synthesized from (S)- and (R)-N-Bocserine methyl esters (Boc: tert-butyloxy-carbonyl). The use of these compounds as chiral building blocks has been demonstrated in the synthesis of α-alkyl α-amino acids by diastereoselective po tassium enolate alkylation reactions and subsequent acid hydrolyses. Theoretical studies were performed to eluci date the stereochemical outcome of both the formation of five-membered cyclic N,O-acetals and the subsequent alkylation process, which occurs with total retention of configuration. This feature could be explained in terms of the high degree of pyramidalization of enolate intermediates. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.