Method for Obtaining Novel Derivatives of Naphthalene for the In Vivo Diagnosis of Alzheimer's Disease
申请人:Carrazana Marquiza Sablón
公开号:US20120321560A1
公开(公告)日:2012-12-20
This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R
1
:-alkylenyl-C(O)NH-alkylenyl-R
3
, -alkylenyl-C(O)O—R
4
, R
3
:—COOH, —OH, —SH, —NH
2
, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R
4
: H, succinimidyl group, R
2
: —H,-alkyl. In II: R
1
: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R
2
: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN)
2
, —HC═CHNO
2
, -alkylenyl-NH
2
, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.
这项发明涉及化学领域,特别是属于芳香双环或萘类别的化合物有机合成领域,用于检测淀粉样蛋白片。这些新的萘衍生物具有一般公式:其中R代表相互独立的基团。在I中:R1:-烷基-C(O)NH-烷基-R3,-烷基-C(O)O—R4,R3:—COOH,—OH,—SH,—NH2,-烷基-NH-烷基-N-二硫代氨基甲酸盐,R4:H,琥珀酰亚胺基团,R2:—H,-烷基。在II中:R1:-烷基,-烷基卤代-烷基羟基-烷基-O-芳基,—O-烷基磺酸酯烷基,R2:-卤代-烷基-O-芳基,-烷基-O-烷基磺酸酯,-烷基卤代-,—CH(O),—HC═C(CN)2,—HC═CHNO2,-烷基-NH2,-烷基-NH-烷基,-烷基-烷基-N-二硫代氨基盐。术语“烷基”和“烷基烯基”指直链或支链脂肪链,最好是1到4个碳原子,卤代指氟、溴或碘。这些化合物是中性的、亲脂性的,具有低分子量,因此它们可以穿过血脑屏障并附着在淀粉样蛋白片上。本发明提供了获得萘衍生物的程序,其产率高,可以实用、经济,并适用于大规模生产。我们不知道本发明中提出的化合物是否已经被先前报道。