ES301713A1 - Procedure for the preparation of new derivatives of tiepine (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Process for the preparation of new tiepine derivatives of the general formula I ** (See formula) ** in which X1 and X2 independently denote chlorine or bromine atoms, Y1, by itself, means hydrogen or a lower alkyl radical, Y2 alone, means hydrogen, or Y1 and Y2 mean together an additional link R1 means hydrogen or a lower alkyl radical, R2 means a hydrocarbon radical, saturated aliphatic, lower, R3 means hydrogen or a saturated, lower aliphatic hydrocarbon radical, or R2 and R3 together with the adjacent nitrogen atom, optionally under the inclusion of bivalent oxygen, the imino group or an alkylimino, hydroxyalkylimino or lower alkanoyloxyalkylimino group, as the ring link, form a heterocyclic radical, and n is 0 or 1, and its salts with inorganic and organic acids, characterized in that a compound of the general formula II is reduced in an organic solvent. ** (See formula) ** in which R3 'means hydrogen, or a lower saturated aliphatic hydrocarbon radical, which together with the lower saturated aliphatic hydrocarbon radical R2, and the adjacent nitrogen atom, and optionally under the inclusion of bivalent oxygen, the imino group, or a lower alkylimino group, as link of the ring can form a heterocyclic radical, and X1, X2, Y1, Y2, R1 and n have the significance indicated above, by a complex hydride, if desired, a compound of the general formula I is treated, which contains an imino group, as a ring link, between R2 and R3 ', with a lower alkylene oxide, with a monoester capable of reacting, of a lower alkanole or with an ester capable of reacting a lower alkanoyloxyalkanol if desired, a compound is acylated with a lower hydroxyalkylimino group, as a ring link between R2 and R3 to reach one of such compounds with a lower alkanoyloxy-alkylimino group and, if desired, a compound of the general formula I is converted to a salt with an inorganic or organic acid. (Machine-translation by Google Translate, not legally binding)