1.
Bioorg Med Chem Lett
; 28(8): 1352-1356, 2018 05 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-29548575
RESUMEN
Z-Endoxifen is widely regarded as the most active metabolite of tamoxifen, and has recently demonstrated a 26.3% clinical benefit in a phase I clinical trial to treat metastatic breast cancer after the failure of standard endocrine therapy. Future pharmacological and pre-clinical studies of Z-endoxifen would benefit from reliable and efficient synthetic access to the drug. Here, we describe a short and efficient, stereoselective synthesis of Z-endoxifen capable of delivering multi-gram (37â¯g) quantities of the drug inâ¯>97% purity with a Z/E ratioâ¯>99% after trituration.