Title of article :
Synthesis of (−)-5,8-Dihydroxy-3R-methyl-2R-(dipropylamino)-1,2,3,4-tetrahydronaphthalene: An Inhibitor of β-Amyloid1–42 Aggregation Original Research Article
Author/Authors :
Michael H Parker، نويسنده , , Robert Chen، نويسنده , , Kelly A Conway، نويسنده , , Daniel H.S Lee، نويسنده , , Chi Luo، نويسنده , , Robert E Boyd، نويسنده , , Samuel O. Nortey، نويسنده , , Tina M Ross، نويسنده , , Malcolm C. Scott، نويسنده , , Allen B. Reitz، نويسنده ,
Abstract :
A concise synthesis of the β-amyloid1–42 aggregation inhibitor (−)-5,8-dihydroxy-3R-methyl-2R-(dipropylamino)-1,2,3,4-tetrahydronaphthalene [(−)-] has been developed. The key step is a regio- and diastereoselective hydroboration-amination sequence to convert alkene into amine . Enantiomeric resolution was achieved by recrystallization of amine as the dibenzoyl-d-tartaric acid salt. Hydroquinone is a potent inhibitor of the fibrillar aggregation of β-amyloid as determined in two different assay systems.
