Yu Donna D, Forman Barry M
Division of Molecular Medicine, The Beckman Research Institute, The City of Hope National Medical Center, Duarte, California 91010, USA.
J Org Chem. 2003 Nov 28;68(24):9489-91. doi: 10.1021/jo035164n.
A McMurry coupling reaction and selective crystallization were used to develop a simple and efficient two-step synthesis of (Z)-4-hydroxytamoxifen (2a). This compound is an active metabolite of tamoxifen, a selective estrogen receptor (ER) modulator widely used to treat breast cancer. The synthesis employed 1,1-bis(4-hydroxyphenyl)-2-phenylbut-1-ene (1) as a useful building block.
采用麦克默里偶联反应和选择性结晶法，开发了一种简单有效的两步法合成（Z）-4-羟基他莫昔芬（2a）。该化合物是他莫昔芬的活性代谢物，他莫昔芬是一种广泛用于治疗乳腺癌的选择性雌激素受体（ER）调节剂。该合成方法使用1,1-双（4-羟基苯基）-2-苯基丁-1-烯（1）作为有用的结构单元。
