besipirdine

besipirdine Chemische Eigenschaften,Einsatz,Produktion Methoden

• Originator

  Besipirdine,Hoechst-Roussel

• Verwenden

  Alzheimer’s disease treatment (cognition enhancer).

• Manufacturing Process

  Part A: N-Propyl-N-(4-pyridinyl)-1H-indol-1-amine maleate: A solution of N-(4-pyridinyl)-1H-indol-1-amine (6 g) in 25 ml of dimethylformamide was slowly added to an ice-cooled suspension of NaH (1.3 g of 60% NaH dispersion in mineral oil was washed with hexanes, the liquid was decanted and the residual solid was dispersed in 5 ml of dimethylformamide). After anion formation, a solution of 1-bromopropane (4 g) in 5 ml of dimethylformamide was added. After one hour of stirring at ambient temperature, the reaction mixture was stirred with ice-water and extracted with dichloromethane. The organic extract was washed with water and saturated sodium chloride solution, was dried over anhydrous magnesium sulfate, filtered and concentrated to 8 g of oil. This oil was purified by HPLC (silica, ethyl acetate) and thereafter by column chromatography (alumina, ether) to give 6.4 g oil. This oil was converted to the maleate salt and recrystallized from methanol/ether to give 6.8 g of crystals, m.p. 115-116°C.
  Part B: N-Propyl-N-(4-pyridinyl)-1H-indol-1-amine hydrochloride: N-Propyl-N-(4-pyridinyl)-1H-indol-1-amine maleate was converted to the free base by action of alcaline agent. Then the free base oil was converted to the hydrochloride salt which was recrystallized from methanol; m.p. 212-214°C.

• Therapeutic Function

  Cognition activator

besipirdine Upstream-Materialien And Downstream Produkte

besipirdine Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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