METHOD FOR OBTAINING NOVEL DERIVATIVES OF NAPHTHALENE FOR THE IN VIVO DIAGNOSIS OF ALZHEIMER'S DISEASE

The invention relates to chemistry and in particular to the field involved in the organic synthesis of compounds belonging to the category of naphthalene or bicyclic aromatics, used in the detection of amyloid plaques. These novel naphthalene derivatives have general formula: (I), (II), wherein: R represents groups that are independent of one another. In formula (I), R1 represents -alkylenyl-C(O)NH- alkylenyl-R3, -alkylenyl-C(O)O-R4; R3 represents -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-/V- dithiocarbamate of salts of alkaline earth metals; R4 represents H, succinimide group; and R2 represents -H, - alkyl. In formula (II), R1 represents -alkyl, -alkylenyl-halide, -alkylenyl-hidroxyl, -alkylenyl-O- arylsulfonate, alkylenyl-O-alkylsulfonate; R2 represents-halide, -alkylenyl-O-arylsulfonate, - alkylenyl-O-alkylsulfonate, -alkylenyl-halide, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-?/-dithiocarbamate of alkaline salts. The terms "alkyl" and "alkylenyl" refer to linear or branched aliphatic chains, preferably with between 1 and 4 carbon atoms, and the term halide refers to fluorine, bromine or iodine. These compounds are neutral, lipophilic and of low molecular weight, allowing same to pass through the blood-brain barrier and adhere to amyloid plaques. The invention relates to methods for obtaining naphthalene derivatives in good yields, which are practical, economical and can be adapted to larger-scale manufacture. We are not aware of any reference in the prior art to the compounds presented in this application. L'invention concerne la branche de la chimie, et notamment le domaine de la synthèse organique de composés appartenant à la catégorie des composés aromatiques bicycliques ou naphtaléniques, utilisés dans la détection de plaques amyloïdes. Ces nouveaux dérivés de naphtalène sont représentés par les formules générales (I) et (II), dans lesquelles R représente des groupes mutuellement indépendants. Dans la formule (I): R1 est -alkylényl-C(O)NH-alkylényl-R3, -alkylényl-C(O))-R4; R3 est -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-N-dithiocarbamate de sels de métaux alcalino-terreux; R4 est H, un groupe succinimide; R2 est -H, -alkyle. Dans la formule (II): R1 est -alkyle, -alkylényl-haluro, -alkylényl-hydroxylo, -alkylényl-O-arylsulfonate, alkylényl-O-alkylsulfonate; R2 est -haluro, -alkylényl-O-arylsulfonate, -alkylényl-O-alkylsulfonate, -alkylényl-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, -alkylényl-NH2, alkylényl-NH