NEW UREA DERIVATIVE AND ITS PRODUCTION

PROBLEM TO BE SOLVED: To produce the subject new compound having a structure in which one of the N atoms is a constituent component of a piperazine ring and the other N atom is substituted with benzylaminoethyl group and useful for treating dysfunction of a gastrointestinal tract and inflammatory di...

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Hauptverfasser: JASSERAND DANIEL, ANTEL JOCHEN, BRUECKNER REINHARD, BIELENBERG GERHARD-WILHELM, EECKOUT CHRISTIAN, DAVID SAMUEL
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To produce the subject new compound having a structure in which one of the N atoms is a constituent component of a piperazine ring and the other N atom is substituted with benzylaminoethyl group and useful for treating dysfunction of a gastrointestinal tract and inflammatory disorders. SOLUTION: This new compound is a compound represented by formula I (R is H or a lower alkyl; R is H or a halogen; R is H or a lower alkoxy) and its physiologically acceptable acid addition salt, e.g. (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(1H-indol-3-ylmethyl)-4- 2-[N-(2-methoxybenzyl) aminoethyl]-aminocarbonyl}piperazine. The compound represented by formula I is produced by reacting a compound represented by formula II with a reactive carbonyl compound represented by formula III (Y is a leaving group of a primary amine or a secondary amine capable of carrying out nucleophilic substitution), providing a carbamoyl compound and then reacting the resultant compound with a compound represented by formula IV (R is a lower alkyl or an amino- protecting group).