ES437505A1 - Procedure for obtaining morpholine derivatives. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Procedure for obtaining morpholine derivatives, of the formula: **(See formula)** wherein A represents an ethylene (-CH2CH2-) or vinylene (-CH = CH-) radical and X represents a phenyl radical optionally substituted by one or two substituents selected from the group consisting of halogen atoms, alkoxy radicals from 1 to 6 carbon atoms and radicals of 6 to 10 carbon atoms, said aryloxy radicals in turn being optionally substituted by one or two substituents selected from the group consisting of halogen atoms and alkyl radicals of 1 to 4 carbon atoms, and the salts of Pharmaceutically acceptable addition acids thereof, characterized in that it comprises: (a) replacing the radical R1 with hydrogen in a compound of the formula: **(See formula)** wherein R1 is an optionally substituted alkanoyl or alkoxycarbonyl radical of up to 6 carbon atoms, an aroyl, an arylalkyl or aryloxycarbonyl radical of up to 11 carbon atoms or a cyano radical; (b) for those compounds in which A is an ethylene radical, reduce a compound of the formula: **(See formula)** with hydrogen in the presence of a catalyst; (o) for those compounds in which, A is a vinylidene radical, dehydrate a compound of formula: **(See formula)** (d) for those compounds in which A is an ethylene radical, react a compound of formula IV with hydrogen in the presence of a catalyst; (e) cyclizing a compound of the formula: X - A -CHOH.CH2.NH.CH2CH2 - Z wherein Z represents a displaceable halogen atom or sulfonyloxy radical, in the presence of a base; (f) reduce a compound of formula: **(See formula)** (g) for those compounds in which A is an ethylene radical, desulfurize a compound of formula: **(See formula)** (h) for those compounds in which A is a transvinylene radical, isomerize a compound of formula: **(See formula)** (i) for those compounds in which A is a vinyl radical, remove the hydrogen and halogen elements from a compound of formula: **(See formula)** where Y is a halogen atom; or (j) for a compound that is an optically active enantiomer, redissolution of the racemic compound of formula I by conventional means, or by using procedures (a) to (i) in which the intermediate of formulas II, III, IV, V, VI, VII, VIII or IX is a dissolved isomer. (Machine-translation by Google Translate, not legally binding)