ES427560A1 - Procedure for the preparation of new derivatives of cyclobutane. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Procedure for the preparation of new cyclobutane derivatives of the general formula **(See formula)** where R1 to R3, which may be the same or different, signify hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alcohol radicals with 1 to 6 carbon atoms, alkoxy radicals with 1 to 3 carbon atoms. carbon or two of the radicals R1 to R3 together signify a methylenedioxy group; R4 signifies a hydrogen atom or an alcohol radical with 1 or 2 carbon atoms; R5 signifies a hydrogen atom or an alcohol radical with 1 to 3 carbon atoms; and R6 means a phenyl radical that can be monosubstituted or disubstituted with a halogen atom, trifluoromethyl groups, hydroxy, nitro, amino, benzyloxy, acyloxy, alcohol radicals with 1 to 3 carbon atoms, alkoxy radicals with 1 to 3 carbon atoms or alcoholylthio radicals with 1 to 3 carbon atoms, or a pyridyl radical optionally substituted with a halogen atom, a hydroxy, nitro, amino, benzyloxy, acyloxy, carboxy group, a carbalkoxy radical with 1 to 3 carbon atoms, a radical alcohol with 1 to 3 carbon atoms or an alkoxy radical with 1 to 3 carbon atoms, as well as its salts with physiologically compatible organic or inorganic acids or bases, characterized in that a compound of the general formula II is reacted **(See formula)** wherein R1 through R4 are as initially defined and X represents a halogen atom or the para-toluenesulfonyloxy radical, with an amine of the general formula III, R6-NH2 wherein R6 is as initially defined and, if a compound of the general formula I, which is substituted with one or more halogen atoms, is obtained according to the method, it is then dehalogenated if desired, and/or a cis/trans mixture, obtained, of a compound of the general formula I is, if desired, subsequently divided into the corresponding cis and trans compounds, and/or a compound obtained of the general formula I in which the radicals R1 to R3 signify acyloxy groups and/or the radical R6 contains an acyloxy and/or carbalkoxy group, is subsequently transformed into the corresponding compound with free hydroxy or carboxyl groups, and/or a compound obtained of the general formula I, which contains free hydroxy groups, is acylated or alcoholized if desired below, and/or a compound of the general formula I obtained is transformed, if desired, with organic or inorganic acids or bases, into their physical salts iologically compatible. (Machine-translation by Google Translate, not legally binding)