1227685-11-1Relevant articles and documents
Process development and scale-up of a β-secretase inhibitor via a stereospecific jocic reaction
Henegar, Kevin E.,Lira, Ricardo,Kim, Hui,Gonzalez-Hernandez, Juan
, p. 985 - 990 (2013/08/23)
A scalable process for the synthesis of a spiropiperidine β-secretase inhibitor is described. Key stereochemical transformations utilized are a diastereoselective trichloromethyl addition followed by an unprecedented stereospecific Jocic reaction with an aniline nucleophile. Simplified processing was developed for a Dieckmann cyclization/decarboxylation sequence to give a process suitable for the production of kilogram quantities of API.
LACTAMS AS BETA SECRETASE INHIBITORS
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Page/Page column 28-29, (2013/02/28)
Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermedia