113741-17-6Relevant articles and documents
Novel imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them
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, (2008/06/13)
The present invention relates to novel imidazolidine derivatives of formula I, wherein A, E, Z, R1, R2, R3, R4 and R5 have the meanings indicated in the claims. The compounds of formula I are valuable pharmaceutical active compounds which are suitable, for example, for the treatment of inflammatory diseases, including rheumatoid arthritis, or allergic diseases. The compounds of formula I are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the treatment of diseases which are caused by an undesired extent of leukocyte adhesion and/or leukocyte migration or are associated therewith or in which cell-cell or cell-matrix interactions which are based on the interactions of VLA-4 receptors with their ligands play a role. The invention furthermore relates to processes for the preparation of the compounds of formula I, their use and pharmaceutical preparations which contain compounds of formula I.
The preparation of enantiomerically pure cyclopropylalanine
Boaz, Neil W.,Debenham, Sheryl D.,Large, Shannon E.,Moore, Mary K.
, p. 3575 - 3580 (2007/10/03)
Single enantiomer cyclopropylalanine (>99.9% ee) and various derivatives were prepared using an asymmetric hydrogenation approach with a rhodium catalyst based on the methyl BoPhoz ligand. N-Boc cyclopropylalanine benzyl ester was the preferred derivative
Phosphinoferrocenylaminophosphines as novel and practical ligands for asymmetric catalysis
Boaz, Neil W.,Debenham, Sheryl D.,Mackenzie, Elaine B.,Large, Shannon E.
, p. 2421 - 2424 (2007/10/03)
(Matrix Presented) A new series of ligands with a novel phosphine-aminophosphine ligation design as depicted in structure 1 has been prepared on a ferrocenylethyl backbone. These BoPhoz ligands of structure 2 have afforded exceedingly high activity and enantioselectivity in the rhodium-catalyzed asymmetric hydrogenation of dehydro-α-amino acid derivatives, itaconic acids, and α-ketoesters. These air-stable ligands are readily prepared from cost-effective and non-pyrophoric intermediates.