Method For The Production of Praziquantel and Precursors Thereof
AssigneeMerck Patent GmbH
InventorsDavid MAILLARD, Andreas WAECHTLER, Jeremy MAURIN, Ewgenij WAKARESKO, Christian JASPER
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Abstract
The present invention relates to methods for the production of enantiopure or enantioenriched Praziquantel precursors and to methods for the production of enantiopure or enantioenriched Praziquantel comprising the methods for the production of the Praziquantel precursors. The present invention further relates to compounds or intermediates useful in such methods.
Claims20
Method for the production of enantiopure or enantiomerically enriched (R)-Praziquanamine comprising the following step:
- Chiral resolution of a mixture of the enantiomers (S)-(I) and (R)-(I) of Praziquanamine,
- via precipitation of a diastereomeric salt formed by one of the enantiomers (S)-(I) or (R)-(I) with an enantiopure or enantioenriched chiral 2-aryl-propionic acid containing at least 14 C-atoms.
Method for the production of enantiopure or enantiomerically enriched (R)-Praziquanacetamide comprising the following step:
- Chiral resolution of a mixture of the enantiomers (S)-(II) and (R)-(II) of N-substituted Praziquandiamine
- via precipitation of a diastereomeric salt formed by one of the enantiomers (S)-(II) or (R)-(II) with an enantiopure or enantioenriched chiral 2-aryl-propionic acid containing at least 14 C-atoms, wherein R2 denotes denotes tert.-butyloxycarbonyl, benzoyl, cyclohexanoyl or acetyl.
Diastereomeric salt comprising (R)-Praziquanamine and (S)-Naproxen or a solvate thereof or (R)-Praziquanacetamide and (S)-Naproxen or (S)-Ketoprofen or a solvate thereof.
Dependencies are inferred from the claim text.