| abstract |
The present invention concerns a branch of chemistry, particularly in the field of organic synthesis of compounds belonging to the category of bicyclic or naphthalenic aromatics, used in the detection of amyloid plaques. These new naphthalene derivatives belong to the general formula (I), (II). Where R represents mutually independent groups. In I: R1: - alkylenyl-C (O) NH-alkylenyl-R3, -alkylenyl-C (O) O-R4; R3: -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-N-dithiocarbamate of alkaline earth metal salts. R4: succinimidyl group; R2: -H, -alkyl. In II: R1: -alkyl, -alkylenyl-halide, -alkylenyl-hydroxyl, -alkylenyl-O-arylsulfonate, alkylenyl-O-alkylsulfonate; R2: -halide, -alkenyl-O-arylsulfonate, -alkylenyl-O-alkylsulfonate, -alkenyl-halide, -CH (O), -HC = C (CN) 2, -HC = CHNO2, alkenyl-NH2, -alkenylenyl -NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate of alkaline salts. The terms "alkyl" and "alkylenyl" refer to straight or branched aliphatic chains, preferably 1 to 4 carbon atoms and the term halide refers to fluorine, bromine or iodine. These compounds are neutral, lipophilic with low molecular weight, and therefore they cross the blood-brain barrier and attach to amyloid plaques. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical (...). |