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 r...
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Zusammenfassung: | 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.
Esta invención se relaciona con la rama de la Química, en particular con el campo de la síntesis orgánica de compuestos que pertenecen a la categoría de aromáticos bicíclicos o naftalénicos, utilizados en la detección de placas amiloideas. Estos nuevos derivados de naftaleno tienen fórmula general: (I), (II). Donde R representa a grupos independientes entre sí. En I: R1: -alquilenil-C(O)NH- alquilenil-R3, -alquilenil-C(O)O-R4; R3: -COOH, -OH, -SH, -NH2, -alquil-NH, -alquil-/V- ditiocarbamato de sales de metales alcalino térreo; R4: H, grupo succinimido; R2: -H, - alquil. En II: R1: -alquilo, -alquilenil-haluro, -alquilenil-hidroxilo, -alquilenil-O- arilsulfonato, alquilenil-O-alquilsulfonato; R2:-haluro, -alquilenil-O-arilsulfonato, - alquilenil-O-alquilsulfonato, -alquilenil-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alquilenil-NH2, -alquilenil-NH-alquil, -alqu¡lenil-alquil-?/-ditiocarbamato de sales alcalina |
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