Issue in Honor of Prof. Sándor Antus ARKIVOC 2004 (vii) 53-59
ISSN 1424-6376 Page 53
©
ARKAT USA, Inc
Time dependent efficiency of optical resolution of aminooxiranes
with O,O'-dibenzoyl-(R,R)-tartaric acid
Ferenc Faigl
* a,b
, Angelika Thurner
b
, Ferenc Farkas
a
, Ágnes Proszenyák
a
, Michela
Valacchi
c
, and Alesandro Mordini
c
a
Department of Organic Chemical Technology, Budapest University of Technology and
Economics, H-1521 Budapest, Hungary
b
Research Group for Organic Chemical Technology, Hungarian Academy of Sciences, H-1521
Budapest, Hungary
c
Istituto di Chimica dei Composti Organometallici, Dipartimento di Chimica Organica “U.
Schiff”, Via della Lastruccia 13 I-50019-Sesto Fiorentino, Firenze Italy
E-mail: ffaigl@mail.bme.hu
Dedicated to Professor Sándor Antus on his 60
th
birthday
(received 03 Oct 03; accepted 04 Dec 03; published on the web 06 Dec 03)
Abstract
Crystallization time dependent efficiencies of optical resolutions of two aminooxirane
derivatives have been investigated. Time-scaled experiments demonstrated that efficient chiral
discrimination of aminooxirane enantiomers by the resolving agent develops in slow, diffusion
controlled exchange of the enantiomers between the solution and the precipitated salt of an
enantiomeric mixture and the resolving agent. Comparison of the determined absolute
configurations of the resolved aminooxiranes showed that quasi enantiomers of the structurally
similar two model compounds crystallized with the same resolving agent from ethyl acetate.
Keywords: Optical resolution, chiral amino oxiranes, chiral discrimination, diastereoisomeric
salt formation
Introduction
Optical resolution via diastereoisomeric salt formation is known as a thermodynamically
controlled process.
1
It means that the enantiomeric excess found in the crystallized salt has been
determined by the solubility and dissociation constants of the two diastereoisomeric salts and the
initial concentrations of the racemate and the resolving agent.
2
There are two classical methods to increase the enantiomeric excess of a diastereoisomeric
salt: (a) recrystallization of the salt or (b) repeated resolution of the non racemic enantiomeric