PROCESS FOR PREPARING 3-SUBSTITUTED PYRROLIDINE COMPOUNDS
Disclosed is a process for preparing 3 -substituted pyrrolidine compounds of formula (VII) or salts thereof, wherein R1 is described herein, which are intermediate compounds useful for the synthesis of darifenacin which is indicated for the treatment of overactive bladder with symptoms of urge, urinary incontinence, and the like, and pharmaceutically acceptable salts thereof. Also disclosed is a process for preparing darifenacin and pharmaceutically acceptable salts thereof.
The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R1 to R4 are as defined in the description and claims. The compounds of the present invention are us
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N-Substituted-3-arylpyrrolidines: Potent and Selective Ligands at Serotonin 1A Receptor
3-Arylpyrrolidines are synthesized through the coupling of N-benzyl-3-(methanesulfonyloxy)pyrrolidine with diarylcuprates. Pharmacological evaluation of a series of N-substituted-3-arylpyrrolidines toward several neurotransmitter receptors indicated that some of them are good ligands for serotonin 1A receptor. Particularly, N-pyrrolidines were found to be potent and selective ligands. A preliminary biological evaluation for several selected compounds indicated that they are potentially effective antianxiety and antidepressant agents.