BASISK SUBSTITUEREDE 2-CARBALKOXYAMINO-BENZIMIDAZOLYL-5(6)-PHENYLETHERE OG -KETONER SAMT DERES FREMSTILLING OG ANVENDELSE

Procedure for the preparation of basic radical-substituted 2-carbalkoxyamino-benzimidazolyl-5 (6) -phenyl ethers and ketones of the formula (1) **(See formula)** where R3 signifies an alcohol with 1 to 4 carbon atoms, X signifies oxygen, sulfur or (see formula), Y signifies a straight or branched ch...

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Hauptverfasser: LOEWE H, DYWEL D, KIRSCH R, URBANIETZ J
Format: Patent
Sprache:dan
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Zusammenfassung:Procedure for the preparation of basic radical-substituted 2-carbalkoxyamino-benzimidazolyl-5 (6) -phenyl ethers and ketones of the formula (1) **(See formula)** where R3 signifies an alcohol with 1 to 4 carbon atoms, X signifies oxygen, sulfur or (see formula), Y signifies a straight or branched chain alcoholic group having 1 to 4 carbon atoms, and R1 and R2 signify a alcohol radical with 1 to 4 carbon atoms, both radicals R1 and R2 being able to signify, together with the N atom that carries them, also the pyrrolidine, piperidine, morpholine or thiomorpholine ring, and their salts with a physiologically acid tolerable, characterized in that an o-phenylenediamine derivative of the formula (2) **(See formula)** wherein R1, R2, X and Y have the same meanings as in formula (1), a) is condensed with an alcoholic S-methyl-thiourea-carboxylate of formula (3), **(See formula)** in which R3 has the same meaning as in formula (1), or b) is condensed with a cyanamidocarboxylate of formula (4) **(See formula)** in which R3 has the same meaning as in formula (1), in each case in a pH range of 1 to 6, or c) it is reacted with a bis-alcoholylthio-methylene-amino-formic or bis-arylthio-methylene-aminoformic acid of the formula (5) **(See formula)** wherein R6 has the meaning given for R3 in formula (1), and R4 and R5 are the same or different and signify an alcohol radical with 1 to 4 carbon atoms, an alkenyl radical with 3 to 5 carbon atoms, a cyclohexyl radical or an optionally substituted phenyl or benzyl radical of the formulas (6) or (7) respectively, **(See formula)** representing the Z, independently of each other, halogen, methyl or nitro, or in which R4 and R5 can also be, united to form a ring containing 2 or 3 methylene groups, and in which n means the numbers 0, 1 or 2, and because, optionally, a compound of formula (1) is reacted with a physiologically tolerable acid. (Machine-translation by Google Translate, not legally binding)