An expeditious synthesis of tamoxifen, a representative SERM (selective estrogen receptor modulator), via the three-component coupling reaction among aromatic …

…, T Yokoyama, A Sasaki, T Orikasa, T Miyamoto…

文献索引：Shiina, Isamu; Sano, Yoshiyuki; Nakata, Kenya; Suzuki, Masahiko; Yokoyama, Toshikazu; Sasaki, Akane; Orikasa, Tomoko; Miyamoto, Tomomi; Ikekita, Masahiko; Nagahara, Yukitoshi; Hasome, Yoshimune Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 24 p. 7599 - 7617

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被引用次数: 16

摘要

Two new synthetic pathways to the anti-cancer agent tamoxifen and its derivatives were developed. The first route involved the aldol reaction of benzyl phenyl ketone with acetaldehyde followed by Friedel–Crafts substitution with anisole in the presence of Cl2Si (OTf) 2 to produce 1, 1, 2-triaryl-3-acetoxybutane, a precursor of the tamoxifen derivatives. The second one utilized the novel three-component coupling reaction among aromatic ...