- Process for the preparation of eszopiclone
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The invention relates to a process for making of 6-(5-chloro-2-pyridinyl)-6,7-dihydro-7-oxo-5H-pyrrolo-[3,4-b] pyrazin-5-yl-4-methyl piperazine-1-carboxylate, also known as zopiclone. The invention further describes an effective method for resolving of zopiclone into its enantiomers (eszopiclone and (R)-zopiclone) and also provides a method of recycling of (R)-zopiclone.
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Page/Page column 4-5
(2008/12/06)
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- IMPROVED PROCESS FOR THE PREPARATION OF ZOPICLONE AND IT'S ENANTIOMERICALLY ENRICHED ISOMER
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Present invention relates to an improved process for the preparation of Zopiclone and its enantiomerically enriched isomer (Eszopiclone). 6-(5-Chloropyridin-2- yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo [3,4-b] pyrazine is reacted with 1-chloro- carbonyl-4-methylpiperazine in the presence of alkali earth metal carbonates, hydroxides or oxides in a solvent medium to give Zopiclone. It is reacted with optically active acid in a mixture of water and water miscible organic solvent followed by work up to give Eszopiclone. The present invention also relates to process for the conversion of (R) or (S) Zopiclone to 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydro- pyrrolo- [3,4-b] - pyrazine of the intermediate which can be converted to racemic Zopiclone.
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Page/Page column 8
(2008/12/08)
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- CYCLIC IMINOCARBAMATES AND USE THEREOF
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The invention relates to novel cyclic iminocarbamates of formula (I), wherein R1, R2, R3, A, Z and n have the meaning cited in the description, to a method for the production thereof, to the use thereof for treating and/or for the prophylaxis of illnesses, and to the use thereof in the production of medicaments for treating and/or for the prophylaxis of diseases, in particular of thromboembolic diseases.
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Page/Page column 28-29; 17
(2010/11/08)
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- PYRAZINE DICARBOXAMIDES AND THE USE THEREOF
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The invention relates to novel pyrazine dicarboxamides, methods for the use thereof, their use for treating and/or preventing diseases as well as to their use for producing medicaments for treating and/or preventing diseases, particularly thromboembolic disorders.
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Page/Page column 33-34
(2010/11/08)
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