Details for Patent: 7,183,410
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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 |
Application Number: | 10/210,474 |
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. |