Generated: April 30, 2017
|Title:||Stable polymorph of flibanserin|
|Abstract:||The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.|
|Inventor(s):||Bombarda; Carlo (Chester, VA), Dubini; Enrica (Milan, IT), Ezhaya; Antoine (Milan, IT), Schneider, legal representative; Margarete (Ingelheim, DE), Schneider, deceased; Heinrich (Ingelheim, DE)|
|Assignee:||Bidachem S.p.A. (Fornovo San Giovanna, IT)|
|Filing Date:||Aug 01, 2002|
|Claims:||1. A process for preparing form A of flibanserin 1 having an endothermic maximum at about 161.degree. C. which occurs during thermal analysis using DSC, ##STR00003## said process comprising: (a) reacting a benzimidazolone 2 ##STR00004## wherein R denotes a suitable amino protecting group, with a piperazine 3 ##STR00005## wherein X is a leaving group selected from chlorine, bromine, iodine, methanesulphonate, trifluoromethanesulphonate and para-toluenesulphonate, in a suitable solvent selected from water, alcohols, mixtures of water with alcohols, polar aprotic solvents and mixtures of polar aprotic solvents with water, in the presence of a suitable base, and (b) cleaving the amino protecting group R under suitable cleaving conditions. |
2. A process according to claim 1, wherein the reaction of 2 with 3 is conducted at a temperature of at least 50.degree. C.
3. A process according to claim 2, wherein heating is conducted for about 10 minutes to about 12 hours.
4. A process for preparing flibanserin 1 comprising form A having an endothermic maximum at about 161.degree. C. which occurs during thermal analysis using DSC, ##STR00006## said process comprising: (a) reacting a benzimidazolone 2 ##STR00007## wherein R denotes a suitable amino protecting group, with a piperazine 3 ##STR00008##
5. A process according to claim 4, wherein the reaction of 2 with 3 is conducted at a temperature of at least 50.degree. C.
6. A process according to claim 5, wherein heating is conducted for about 10 minutes to about 12 hours.
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