The present invention relates to compounds of formula (I): useful in treating Alzheimer’s disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer’s disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Synthesis of α,α-disubstituted α-amino acid amides by phase-transfer catalyzed alkylation
作者:Bernard Kaptein、Wilhelmus H.J. Boesten、Quirinus B. Broxterman、Hans E. Schoemaker、Johan Kamphuis
DOI:10.1016/s0040-4039(00)61112-7
日期:1992.9
α,α-Disubstituted α-amino acid amides were prepared in 17–86% chemical yield by the phase-transfer catalyzed alkylation of N-benzylidene α-H aminoacid amides, followed by weak acidic hydrolysis of the Schiffbases.