VTP-36951 / AbbVie - LARVOL DELTA

Synthesis of Beta-Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitors BI 1147560 and BI 1181181 Labeled with Carbon-14 and Deuterium. (PubMed, J Labelled Comp Radiopharm) - "The use of advanced key chiral intermediates like 3 and 5 shortened the carbon 14 syntheses of these two compounds to five and six steps respectively and helped in preparing them with very high chemical purity and enantiomeric excess without deviating from the process chemistry route. For the deuterium synthesis, oxetan-3-ylmethanamine [ H ]-7 and 2-fluoro-2-methylpropan-1-amine [ H ]-9 were prepared then used with the chiral intermediate 5 to furnish deuterium labeled 1 and 2 respectively."

Journal • Alzheimer's Disease • CNS Disorders • APP