Process for the preparation of (s)- naproxen 4-nitrooxybutyl ester
AssigneeNicox S.A.
InventorsAldo BELLI, Vincenzo CANNATA, Telly FONDUCA, Martin HEDBERG, Andreas WESTERMARK, Marco VILLA
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Abstract
The present invention relates to a new process for the preparation of the (S)-naproxen 4-nitrooxybutyl ester and to new intermediates obtained and used therein. The invention further relates to the use of the new intermediates for the manufacturing of pharmaceutically active compounds such as (S)-naproxen 4-nitrooxybutyl ester. The invention also relates to the use of (S)-naproxen 4-nitrooxybutyl ester prepared according to the process of the present invention for the manufacturing of a medicament for the treatment of pain.
Claims19
A process for the preparation of (S)-naproxen 4-nitrooxybutyl ester (IV)
- comprising
- 1b) reacting (S)-naproxen with a compound of formula II,
- wherein R1 and R2 are both H, to obtain a compound of formula III,
- and thereafter,
- is 1c) reacting the compound of formula III with RSO2Cl to give a compound of formula I,
- wherein
- R is C1-C4 alkyl, phenyl, phenylmethyl, C1-C4 alkylphenyl, halophenyl, nitrophenyl, halogen, CF3 or n-C4F9, and the halo or halogen is fluoro, chloro or bromo,
- and
- 2) reacting the compound of formula I with a nitrate source optionally in the presence of a solvent to obtain (S)-naproxen 4-nitrooxybutyl ester.
Dependencies are inferred from the claim text.