Process of making benzodiazocines

Details Process of making benzodiazocines Process of making benzodiazocines

C - Chemistry, Metallurgy

07

D

260/237.75

C07D 245/06 (2006.01)

Patent

CA 1064028

ABSTRACT OF THE DISCLOSURE A process or making benzodiazocine derivatives of the formula Image I wherein R1 is hydrogen, lower alkyl which may be a straight or branched chain with 1 to 6 carbon atoms and may be substituted by halogen, lower alkoxy with at most 4 carbon atoms or phenyl radi- cal, or a cyclic alkyl with 3 to 6 carbon atoms, R2 is a halo, hydroxyl, acetoxy or benzoxy radical, R3 is phenyl or phenyl sub- stituted with one to three member of the group of halogen, alkyl, alkylthio, alkoxy, the alkyl, alkylthio or alkoxy moities of which have at most 4 carbon atoms, or phenyl substituted with a nitro or trifluoromethyl alone or together with one or two of the above sub- stituent, or an ethylenedioxyphenyl, R4 and R5 are each of a radi- cal of the group consisting of hydrogen, halogen, alkyl, alkoxy or alkylthio, the alkyl, alkoxy or alkylthio moities of which have at most 4 carbon atoms, or a trifluoromethyl radical, or together an ethylenedioxy radical; or a pharmaceutically acceptable acid addi- tion salt of said benzodiazocine derivatives of the formula I, said process comprising heating an acyldiamine having the formula Image II in which R is a hydroxy, acetoxy, or benzoxy radical, and R1, R3, R4 and R5 have the same significance as before, with a phosphorus oxyhalide in an inert solvent at a temperature between 50 and 100°C, when the R radical is a hydroxyl radical for making a benzodiazocine derivative of the formula I wherein R2 is halogen, and at a tempera- ture between 50 and 150°C when the R radical is an acetoxy or benzoxy radical for making a benzodiazocine derivative of the formula I wherein R2 is acetoxy or benzoxy, and hydrolyzing the benzodiazocine derivative wherein R2 is acetoxy or benzoxy to a benzodiazocine derivative of the formula I wherein R2 is hydroxy, treating the formula I compound obtained with an acid to convert it into a pharmaceutically compatible acid addition salt thereof, or liberating a base of formula I from its acid addition salt. The invention also embraces benzodiazocine compounds as shown in above formula I whenever made by the above process.

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