134420-93-2Relevant articles and documents
Practical, highly enantioselective chemoenzymatic one-pot synthesis of short-chain aliphatic β-amino acid esters
Wei?, Markus,Gr?ger, Harald
experimental part, p. 1251 - 1254 (2009/09/06)
A practical, highly enantioselective method for the synthesis of short-chain aliphatic β-amino acid esters was developed starting from prochiral and easily accessible substrates. This chemoenzymatic approach is based on a nonenzymatic aza-Michael addition
Process for producing either optically active n-substituted beta-amino acid and optically active n-substituted beta-amino acid ester or optically active n-substituted 2-homopipecolic acid and optically active n-substituted 2-homopipecolic acid ester
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, (2008/06/13)
The present invention discloses a process which comprises selectively hydrolyzing one enantiomer of racemic mixtures of an N-substituted β-amino acid alkyl ester or N-substituted 2-homopipecolic acid ester represented by the formula (I): wherein Ar, Rsup
GABA-uptake inhibitors: Construction of a general pharmacophore model and successful prediction of a new representative
N'Goka,Schlewer,Linget,Chambon,Wermuth
, p. 2547 - 2557 (2007/10/02)
A model for the pharmacophore of GABA-uptake inhibitors was established using published structure-activity data and molecular modeling. The model accounted for the activities of different classes of GABA-uptake inhibitors. Analogues of guvacine substituted at position 6 were synthesized in order to confirm the model. 6-(3,3-Diphenylpropyl)guvacine (30f), which fit well with the pharmacophore, had an in vitro IC50 of 0.1 μM. This value is as good as those of the best GABA-uptake inhibitors known today.
