Process for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl) acetylguanidine derivatives
AssigneeSanofi-Aventis Deutschland GmbH
InventorsGerrit Schubert, Joerg Rieke-Zapp, Johannes Keil, Heinz-Werner Kleemann, Reda Hanna, Bao-Guo Huang, Xiao-Dong Wu, Yves Gouraud
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Abstract
The present invention relates to processes for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetylguanidine derivatives of the formula I via 3-hydroxy-2,3-dihydro-1H-isoindol-1-one derivatives or 3-(2-carbamoylphenyl)-acrylic ester derivatives as intermediates, to a process for optical resolution, and to intermediates of the process according to the invention.
Claims9
A compound of the formula XVa or XVb
- wherein
- R1 and R2
- are each independently hydrogen, F, Cl, trifluoromethoxy, 2,2,2-trifluoroethoxy, trifluoromethyl, 2,2,2-trifluoroethyl or alkyl having 1, 2, 3 or 4 carbon atoms;
- R3 is Alk-R4, trifluoromethyl, alk is alkyl having 1, 2, 3 or 4 carbon atoms;
- R4 is hydrogen, trifluoromethyl or cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms;
- R* is
- R8 is alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms or phenyl which is unsubstituted or substituted by 1, 2 or 3 substituents from the group of F, Cl, Br, I, alkyl having 1, 2, 3 or 4 carbon atoms or alkoxy having 1, 2, 3 or 4 carbon atoms.
(S)-N-{2-[3-oxo-2-(2,2,2-trifluoroethyl)-6-trifluoromethyl-2,3-dihydro-1H-isoindol-1-yl]acetyl}guanidine hydrogenfumarate hydrate of the formula XVI
Dependencies are inferred from the claim text.