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. 2016 Jul 20;4(3):15. doi: 10.3390/biomedicines4030015

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© 2016 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).

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Scheme 1 — Synthesis of endoxifen 11 and hydroxyendoxifen derivative 12. Reagents and conditions: (i) TBDMS-Cl, Imidazole, DMF; (ii) Zn, TiCl₄, THF; (iii) BrCH₂CH₂Br, NaOH (aq.), (nBu)₄NHSO₃; (iv) CH₃NH₂, sealed tube, 60 °C; (v) TBAF, THF. (TBDMS = tert-Butyldimethylsilyl).