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A Multi-Gram-Scale Stereoselective Synthesis of Z-endoxifen

A Multi-Gram-Scale Stereoselective Synthesis of Z-endoxifen

Lech-Gustav Milroy, Bartjan Koning, Daphne S V Scheppingen, Nynke G L Jager, Jos H Beijnen, Jan Koek, Luc Brunsveld

Bioorg Med Chem Lett. 2018 May 1;28(8):1352-1356.

PMID: 29548575

Abstract:

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 (37 g) quantities of the drug in >97% purity with a Z/E ratio >99% after trituration.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP112093284	(Z)-Endoxifen		112093-28-4	Price

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