Fremgangsmåde til fremstilling af imidazo-benzodiazepin-derivater

Prepn. of 4H-imidazo(1,5-a)(1,4) -benzodiazepine derivs. of formula (I) and their salts comprises decarboxylation of a cpd. of type (II) at high temp. and high pressure in the presence of an organic solvent: R = Ph (opt. mono- or di-substd.); R = H, halo, NO2, CN, CF3 or lower alkyl; R , R = H or lo...

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Hauptverfasser: SCHMITT, SIEGFRIED, BENDER, KARL-HEINZ, FROOM, MANFRED, BREUNINGER, MANFRED, STEINER, KURT
Format: Patent
Sprache:dan
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Zusammenfassung:Prepn. of 4H-imidazo(1,5-a)(1,4) -benzodiazepine derivs. of formula (I) and their salts comprises decarboxylation of a cpd. of type (II) at high temp. and high pressure in the presence of an organic solvent: R = Ph (opt. mono- or di-substd.); R = H, halo, NO2, CN, CF3 or lower alkyl; R , R = H or lower alkyl. PREFERRED ALERT - Pref. (I) is 8-chloro-6-(2-fluorophenyl) -1-methyl -4H-imidazo(1,5-a)(1,4) -benzodiazepine, continuously mfd. at 150-350 (pref. 250-350) degrees C and 50-150 (pref. 90-110) bar in n-butanol, n-butylacetate, acetic acid ester, EtOH, ethylene glycol, hexane, isopropylacetate, n-propanol, tetralin or toluene (pref. n-butanol). Prod. is initially recrystallised from n-butanol, butylacetate, tert.-butylmethylether, EtOH, ethylacetate or isopropylacetate (pref. isopropylacetate) and then from EtOH.