Process for the resolution of nefopam
A process for increasing the optical purity of a mixture of enantiomers of nefopam uses a substantially single enantiomer of a O,O-diaroyltartaric acid as a resolving agent, via a bisnefopam salt of the acid. This salt is new.
1. A process for increasing the optical purity of a mixture of enantiomers of nefopam by using a substantially single enantiomer of a O,O-diaroyltartaric acid as a resolving agent, via a bisnefopam salt of the acid.
2. The process according to claim 1 , for preparing a substantially single enantiomer of nefopam by means of resolution of racemic nefopam.
3. The process according to claim 1 , for preparing a substantially single enantiomer of nefopam, which comprises reverse resolution of racemic nefopam, using sequentially a single enantiomer of a O,O-dibenzoyltartaric acid and men the other enantiomer.
4. The process according to claim 1 , for preparing substantially single enantiomer (+)-nefopam, which uses O,O-dibenzoyl-L-tartaric acid as the resolving agent.
5. The process according to claim 1 , for preparing substantially single enantiomer (−)-nefopam, which uses O,O-dibenzoyl-D-tartaric acid as the resolving agent.
6. The process according to claim 1 , which is conducted in a solvent selected from alcohols, esters, ketones and halogenated solvents.
7. The process according to claim 1 , which comprises the further step of conversion of the salt obtained by the resolution to the free base form of nefopam or a pharmaceutically acceptable salt thereof.
8. The process according to claim 1 , wherein the amount of the resolving agent is less than 1 equivalent.
9. The process according to claim 8 , wherein said amount is no more than 0.5 equivalent.
10. A bisnefopam salt of a substantially single enantiomer of a O,O-diaroyltartaric acid.
11. The salt according to claim 10 , wherein the acid is O,O-dibenzoyltartaric acid.