Process for the preparation of novel tripeptide amides acting on the central nervous system

To prepare novel tripeptide amides of the general formula L-Glp-L-His-Y-NH2 (I) in which Y is an L-homoprolyl or D- pipecolyl group, the protected dipeptide hydrazide of the formula Z-L-Gln-L-His-N2H3 (III) in which Z is benzyloxycarbonyl is reacted with nitrites to give the corresponding protected...

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Hauptverfasser: SZIRTES TAMAS, SARKADI ADAM DR, KISFALUDY LAJOS . DR, SPORNY LASZLO DR, PALOSI EVA DR, BALASPIRI LAJOS DR
Format: Patent
Sprache:eng ; ger
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Zusammenfassung:To prepare novel tripeptide amides of the general formula L-Glp-L-His-Y-NH2 (I) in which Y is an L-homoprolyl or D- pipecolyl group, the protected dipeptide hydrazide of the formula Z-L-Gln-L-His-N2H3 (III) in which Z is benzyloxycarbonyl is reacted with nitrites to give the corresponding protected azide, the latter is reacted with an amino amide of the general formula Y-NH2 in which Y has the above meaning, and the glutaminyl group in the resulting tripeptide amide after elimination of the protective group Z is cyclized by heat treatment to give a pyroglutamyl group. The resulting novel tripeptide amides have an effect on the central nervous system.