Patent ID: 6784292
Filing Date: 2004-08-31
Classification: C07D

Abstract:
A process for the production of imidazo[1,2-c][2,3]benzodiazepines of formula (1) in whichR1=is hydrogen, C1-C6-alkyl, nitro, halogen, cyano, C1-C4-alkoxy, â€”CF3, hydroxy or C1-C6-alkanoyloxy, R2 and R3 are the same or different and mean hydrogen, halogen, C1-C6-alkoxy, hydroxy, cyano, C1-C6-alkanoyl, C2-C6-alkynyl, C2-C6-alkenyl; C1-C6-alkyl or C3-C7-cycloalkyl which in each case is unsubstituted or substituted by halogen, hydroxy or C1-6-alkoxy, or an aryl or hetaryl radical which in each case is unsubstituted or substituted by halogen, C1-4-alkoxy or C1-4-alkyl, X=is hydrogen or halogen, Y=is C1-C6-alkoxy, or X and Y together mean â€”Oâ€”(CH2)nâ€”Oâ€”, and n=is 1, 2 or 3, from a phenylacetic acids of formula (4), which process comprises: a) esterifying the phenylacetic and with an alcohol of formula (5a) â€ƒto form a phenylethyl acetate of formula (5) b) condensing the phenylethyl acetate with ammonia or an ammonia donor to form an oxazole of formula (6) c) hydrazinolyzing the oxazole to form the compounds of general formula (1)