Tritiodestannylation. Synthesis of a Specifically Labelled [³H]Tamoxifen

Abstract

The recent development of nonsteroidal antiestrogens has increased the prospects for the management of metastatic breast cancer, the most prevalent malignancy among North American and European women. Of these, clinical results have demonstrated tamoxifen (1) to be at least as effective as conventional hormonal treatment while manifesting much reduced side effects.² As part of a program designed to evaluate inhibitors of aromatization for therapy of breast cancer, we required a tritiated derivative of tamoxifen for pharmacodynamic and radioimmunqassay studies.