Aspartic protease inhibitors via C 1-homologation of peptidic aldehydes and studies on reduced amide isosteres

…, M Brockhaus, M Schütz, R Meusinger, B Schmidt

文献索引：Braun, Hannes A.; Zall, Andrea; Brockhaus, Manfred; Schuetz, Marco; Meusinger, Reinhard; Schmidt, Boris Tetrahedron Letters, 2007 , vol. 48, # 45 p. 7990 - 7993

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被引用次数: 8

摘要

(R)-Configured isophthalic hydroxyethylamines play an important role in the inhibition of β- secretase (BACE1). We present the synthesis of a number of (S)-configured hydroxyethylamine derivatives via 2-iodoethanol intermediates and the comparison with the (R)-analogues. An N-substituted indole was investigated as a substitute for the isophthalamide moiety.