Synthesis of Non-Steroidal Estrogen Receptor Antagonists R1128 A, B, C, and D via an Oxazoline-Promoted Iterative ortho-Lithiation Strategy

T Fukuda, K Fukushima, S Sanai, M Iwao

Index: Fukuda, Tsutomu; Fukushima, Koichiro; Sanai, Susumu; Iwao, Masatomo Bulletin of the Chemical Society of Japan, 2012 , vol. 85, # 1 p. 133 - 135

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Abstract

Division of Chemistry and Materials Science, Graduate School of Engineering, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521 ... Received August 12, 2011 E-mail: iwao@nagasaki-u.ac.jp ... A concise total synthesis of non-steroidal estrogen receptor antagonists R1128 AD (1a1d) has been achieved using iterative ortho-lithiation of 2-(4-methoxyphenyl)-4 ,4- dimethyloxazoline (3) as the key reaction. ... Tamoxifen, a non-steroidal estrogen ...