PROCESS FOR PREPARING BENZOAZEPINE DERIVATIVES

Benzoazepine derivs.[I; R = H, halogen, lower alkyl; X = O, S, -N-R1(R1 = lower alkyl); Y = O, H2 , useful as trnquilizer, were prepd. by reaction of compd. (II) and polyphosphoric acid at 110-130 C. Thus, N-[2-(N-methylanyline)ethyl -3-benzoylpropion amide 4.5 g and polyphosphoric acid 45 g was rea...

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Hauptverfasser: MORIDA IWAO, KISE MASAHIRO, SEDO EISKE
Format: Patent
Sprache:eng
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Zusammenfassung:Benzoazepine derivs.[I; R = H, halogen, lower alkyl; X = O, S, -N-R1(R1 = lower alkyl); Y = O, H2 , useful as trnquilizer, were prepd. by reaction of compd. (II) and polyphosphoric acid at 110-130 C. Thus, N-[2-(N-methylanyline)ethyl -3-benzoylpropion amide 4.5 g and polyphosphoric acid 45 g was reacted at 115-120 C for 3 hr, poured into ice, neutralized with sodium bicarbonate, extracted with chloroform, dried with MgSO4 and recrystallized with water to give 7-methyl-11b-phenyl-1,2,3,5,6,11b-hexahydropyrrolo-[1,2-d [1,4 -benzodia-zepine-3-one 3 g.