This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, l or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.
Synthesis of hindered secondary amines via Grignard reagent addition to ketonitrones
作者:Martin A. Schwartz、Xiufeng Hu
DOI:10.1016/s0040-4039(00)91707-6
日期:1992.3
Grignard reagents add to ketonitrones in a nonpolar solvent to afford N,N-dialkylhydroxylamines in good yields and with little competing proton transfer. Deoxygenation of the crude hydroxylamines with carbon disulfide then completes an efficient general synthetic route to hindered sec-alkyl-tert-alkylamines and to di-tert-alkylamines.