Octahydro-6, 10-dioxo-6h-pyridazino/1,2-a/ /1,2/diazepin-1-carboxylic acid, derivatives, preparation method and use for preparing therapeutically active compounds

A process for the preparation of a compound of the formula

• of SR configuration or a SR+SS mixture wherein R is selected from the group consisting of hydrogen, alkyl of up to 18 carbon atoms and aryl and aralkyl of up to 18 carbon atoms and the —NH2 is free or protected, comprising reacting a compound of the formula
• where Hal is halogen and alk is a alkyl of 1 to 8 carbon atoms with a compound of the formula
• when Aryl is a aryl of up to 14 carbon atoms to form a compound of the formula
• reacting the latter with a basic agent to form a compound of the formula
• optionally subjecting the compound of Formula IV to an alkylating agent to form a compound of the formula
• reacting the latter with a compound of the formula
• wherein Hal1 is halogen, Ar is aryl or aralkyl of up to 18 carbon atoms, R1 is selected from the group consisting of
• Ra, Rb, Rc and Rd are individually selected from the group consisting of alkyl of up to 18 carbon atoms, aryl of up to 18 carbon atoms and monocyclic and polycyclic groups containing at least one nitrogen atom, X is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and aryl of up to 14 carbon atoms and R2 is hydrogen or R1 and R2 together with the nitrogen form a monocyclic or polycyclic with at least one heteroatom to obtain a compound of the formula
• of SR configuration on a SR+SS mixture, reacting the latter with a hydrogenation agent to form a compound of the formula
• of SR configuration or a SR+SS mixture, reacting the latter with a condensation agent to obtain a compound of the formula
• and optionally deprotecting the amine group to obtain a compound of formula I wherein the amine is free.