ES418846A1 - Procedure for the preparation of derivatives of 4-carbamoximetil-1-ftalazona. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

A process for the preparation of 4-carbamoxymethyl-l-phthalazone derivatives that are represented by the general formula I: **(See formula)** Wherein R1 signifies a hydrogen atom or an alcoholic group, R2 signifies a hydrogen atom, an alcoholic group that can be branched or cyclic, or an alkenyl, aryl, aralcohyl, dialkoxylaminoalcoyl, furfuryl, picolyl, or pyridyl group, R3 means a hydrogen atom, an alcoholic group, aryl, carbamoyl, N-alcoholcarbamoyl, N, N-dialkoylcarbamoyl, alcoholylsulfonyl, oarylsulfonyl, R4 signifies a hydrogen or halogen atom, an alcoholic or alkoxy group, R5 signifies a hydrogen atom or halogen, an alcoholic, alkoxy, amino, acylamino, alkoxycarbonyl, or carbamoyl group, and R1 may together with R2 form a divalent alcoholic group which may be interrupted by a heteroatom, and R4 and R5 may be present at any of the C- positions 5, C-6, C-7 or C-8 of the phthalazone nucleus, characterized in that a compound of general formula II is reacted: **(See formula)** wherein R3, R4 and R5 have the same meanings described with respect to formula I, with a compound of general formula III: **(See formula)** wherein A signifies a chlorine atom or an alkoxy, aryloxy, alcoholylthio or arylthio group, and thereafter the intermediate of general formula IV: **(See formula)** wherein R3, R4 and R5 have the same meanings described in formula I and A has the same meanings described in formula III are reacted with ammonia or an amine of general formula V: NHR1R2 V wherein R1 and R2 have the same meanings described in formula I. (Machine-translation by Google Translate, not legally binding)