| 摘要 |
Process for the synthesis of 5-{4-[N-methyl-N- (2-pyridyl)-amino-ethoxy]-5-benzylidene}-thiazolidine-2, 4-dione (INN name: benzylidene-rosiglitazone) of formula (I), which consist of the following steps: (I) Step a) reaction of 2-chloro-pyridine and 2-(N-methylamino)-ethanol Step b) reaction of the obtained compound of formula (III) with 4- 0 fluorobenzaldehyde Step c) reaction of the obtained compound of formula (IV) with thiazolidine-2, 4-dione. (III), ((IV). characterized by - dissolving 4-{2-[N-methyl-N- (2-pyridyl) amino]-ethanol of formula (III) obtained in Step a) in toluene and using it in Step b) without isolation; - reacting the solution of compound of formula (III) in toluene in Step b) with 4-fluorobenzaldehyde in the presence of aqueous alkali hydroxide solution and phase transfer catalyst at 25-50°C; - reacting the solution of the benzaldehyde derivative of formula (IV) obtained in Step b) in toluene in Step c) and isolating the desired product. |
