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

THIS INVENTION RELATES TO CHEMISTRY AND IN PARTICULARL TO THE FIELD INVOLVED IN THE ORGANIC SYNTHESIS OF COMPOUNDS BELONGING TO THE CATEGORY OF NAPHTHALENE OR AROMATIC BICYCLIC, USED IN THE DETECTION OF AMYLOID PLAQUES. THESE NOVEL NAPHTHALENE DERIVATIVES HAVE A GENERAL FORMULA: (I), (II) WHERE R RE...

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Hauptverfasser: PERERA PINTADO,ALEJANDRO, PEREZ MARTINEZ,CARLOS SERAFIN, RODRIGUEZ-TANTY,CHRYSLAINE, PRATS CAPOTE,ANAIS, VALDES SOSA,PEDRO, LÓPEZ BARROSO,ROSA MARIA, SABLÒN CARRAZANA,MARQUIZA, PÉREZ PERERA,RAFAELA, RIVERA MARRERO,SUCHITIL, VÉLEZ CASTRO,HERMÁN
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Sprache:eng
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Zusammenfassung:THIS INVENTION RELATES TO CHEMISTRY AND IN PARTICULARL TO THE FIELD INVOLVED IN THE ORGANIC SYNTHESIS OF COMPOUNDS BELONGING TO THE CATEGORY OF NAPHTHALENE OR AROMATIC BICYCLIC, USED IN THE DETECTION OF AMYLOID PLAQUES. THESE NOVEL NAPHTHALENE DERIVATIVES HAVE A GENERAL FORMULA: (I), (II) WHERE R REPRESENTS GROUPS Y THAT ARE INDEPENDENT OF ONE ANOTHER. IN I: R1 REPRESENT -ALKYLENYL-C(O) NH-ALKYLENYL-R3,-ALKYLENYL-C(O) OR4, R3:-COOH, -OH -SH, -NH2, -NH-ALKYL,-N-LKYL-DITHIOCARBAMATE ALKALINE SALTS OF ALKALINE EARTH METAL SALTS; R4 REPRESENTS H, SUCCINIMIDYL GROUP, AND R2 REPRESENTS -H,ALKYL. IN FORMULA (II): R1 REPRESENTS -ALKYL, -ALKYLENYL-HALIDE, -ALKYLENYL-HYDROXYL, -ALKYLENYL- O-ARYLSULFONATE, -ALKYLENYL-0- ALKYLSULFONATE , R2 REPRESENT -HALIDE, -ALKYLENYL-O-ARYLSULTONATE, -ALKYLENYL-O-ALKYLSULFONATE , - ALKYLENYL-HALIDE-, -CH(O), -HC=C(CN)2, -HC=CHNO2, -ALKYLENYL-NH2, -ALKYLENYL-NH- ALKYL, -ALKYLENYL-ALKYL-N-DITHIOCARBAMATE OF ALKALINE SALTS. THE TERMS "ALKYL" AND "ALKYLENYL" REFER TO LINEAR OR BRANCHED ALIPHATIC CHAINS, PREFERABLY WITH BETWEEN 1 TO 4 CARBON ATOMS, AND THE TERM HALIDE REFERS TO FUORINE, 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 ARMYLOID PLAQUES.THE INVENTION RELATES TO METHODS FOR OBTAINING NAPHTHALENE DERIVATIVES IN GOOD YIELDS, WHICH ARE PRACTICAL, ECONOMICAL AND CAN BE ADAPTED TO A LARGER-SCALE MANUFACTURING. WE ARE NOT UNAWARE OF SNY REFERENCE IN THE PRIOR ART TO THE COMPOUNDS PRESENTED IN THIS APPLICATION.