发明授权
EP0174242B1 Dérivés de 1-(aminophényl)-2-amino-propanone, leur utilisation en thérapeutique et leur procédé de préparation 失效
1-(氨基苯基)-2-氨基丙酮衍生物,其在治疗中的使用及其制备方法

Dérivés de 1-(aminophényl)-2-amino-propanone, leur utilisation en thérapeutique et leur procédé de préparation
摘要:
1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE A 1-(aminophenyl)-2-aminopropanone derivative selected from the group consisting of : a) compounds of the general formula (I) see diagramm : EP0174242,P25,F1 in which X is NH2 , Y is H or a halogen atom, Z is H or a halogen atom, R1 is C1 -C4 alkyl or C3 -C6 cycloalkyl and R2 is H or C1 -C4 alkyl or R1 and R2 , taken together, can form, with the nitrogen atom to which they are bonded, an N-heterocyclic group having from 5 to 7 ring members and which can be substituted, said NR1 R2 groups being selected from the group comprising the pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methylpiperazino and 4-(beta-hydroxyethyl)piperazino, 4-phenylpiperazino and 4-(p-chlorophenyl) piperazino groups ; and b) addition salts thereof. 1. Claims for the Contracting State : AT A method for the preparation of a 1-(aminophenyl)-2-aminopropanone derivative of the general formula : (I) see diagramm : EP0174242,P26,F1 in which X is NH2 , is H or a halogen atom, Z is H or a halogen atom, R1 is C1 -C4 alkyl or C3 -C6 cycloalkyl and R2 is H or C1 -C4 alkyl, or R1 and R2 , taken together, can form, with the nitrogen atom to which they are bonded, an N-heterocyclic group having from 5 to 7 ring members and which can be substituted, said NR1 R2 groups being selected from the group consisting of the pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methylpiperazino and 4-(beta-hydroxyethyl)-piperazino, 4-phenylpiperazino and 4-(p-chlorophenyl) piperazino groups, and addition salts thereof, the said method comprising subjecting a 1-(acetylaminophenyl)-2-amino-propanone derivative of the formula : (II) see diagramm : EP0174242,P26,F2 in which Y, Z, R1 and R2 are defined as indicated above, to a deacetylation reaction with an aqueous solution of HCI, for at least 0,25 hour, at the reflux temperature of the reaction medium, whereby 1 mol of compound II is used for 0,7 to 2 liters of 4 n HCI.
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