Flibanserin, BIMT-17-BS, BIMT-17-药物合成数据库

【药物名称】Flibanserin, BIMT-17-BS, BIMT-17

化学结构式(Chemical Structure):

参考文献No.	19917
标题:	Benzimidazolone derivatives as 5-HT1A agonists and 5-HT2 antagonists
作者:	Turconi, M.; Bietti, G.; Giraldo, E.; Borsini, F.; Bignotti, M. (Boehringer Ingelheim GmbH)
来源:	EP 0526434; JP 1994509575; US 5576318; WO 9303016

合成路线图解说明: Flibanserin may be prepared by reacting 1-(phenylvinyl)-2,3-dihydro-1H-benzimidazol-2-one (I) with 1,2-dichloroethane (II) in the presence of NaH in warm dimethylformamide. The resulting 1-(2-chloroethyl)-2,3-dihydro-1H-benzimidazol-one (III) is in turn coupled with commercially available m-trifluoromethylphenylpiperazine hydrochloride (IV) in the presence of sodium carbonate and catalytic potassium iodide in refluxing ethanol. The crude flibanserin hydrochloride (V) is then dissolved in aqueous ethanol and the pure base is precipitated upon addition of sodium hydroxide.

参考文献No.	439435
标题:	Flibanserin
作者:	Cesana, R.; Borsini, F.; Ladinsky, H.; Ceci, A.; Giraldo, E.; Turconi, M.; Brambilla, A.; Monferini, E.
来源:	Drugs Fut 1998,23(1),9

合成路线图解说明: Flibanserin may be prepared by reacting 1-(phenylvinyl)-2,3-dihydro-1H-benzimidazol-2-one (I) with 1,2-dichloroethane (II) in the presence of NaH in warm dimethylformamide. The resulting 1-(2-chloroethyl)-2,3-dihydro-1H-benzimidazol-one (III) is in turn coupled with commercially available m-trifluoromethylphenylpiperazine hydrochloride (IV) in the presence of sodium carbonate and catalytic potassium iodide in refluxing ethanol. The crude flibanserin hydrochloride (V) is then dissolved in aqueous ethanol and the pure base is precipitated upon addition of sodium hydroxide.