Synthesis of Labeled LY504132, a Selective Estrogen Receptor Modulator

摘要

Selective Estrogen Receptors Modulators (SERM) are a class of compounds that are potentially efficacious in the treatment, e.g., of osteoporosis. LY504132 is a SERM that underwent preclinical ADME investigation. Accordingly, a stable labeled isotopomer was needed for use as an internal standard in LC-MS assays for quantification of LY504132 in biological matrices. The established synthesis for LY504132 provided a building block for the labeled synthesis; slight modifications were necessary to accommodate the insertion of the label. Using piperidine-dn, it was possible to create d)0 labeled 1-(2-chloroethyl)piperidine in two steps. The d_10 label could then be incorporated into the original synthesis. The following poster will detail the creation of the label as well as the complete synthesis of LY504132-[d_10].