… as selective estrogen receptor modulators. Part 2. Process improvement for scale-up of 2, 5, 8-substituted 11, 12-dihydro-5 H-6, 13-dioxabenzo [3, 4] cyclohepta-[1, 2- …

X Li, M Reuman, RK Russell, S Youells…

文献索引：Li, Xun; Reuman, Michael; Russell, Ronald K.; Youells, Scott; Beish, Sandra; Hu, Zhiyong; Branum, Shawn; Jain, Nareshkumar; Sui, Zhihua Organic Process Research and Development, 2007 , vol. 11, # 4 p. 731 - 738

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被引用次数: 10

摘要

An improved, reproducible nonchromatographic process for scale-up synthesis of 2, 5, 8- substituted 11, 12-dihydro-5 H-6, 13-dioxabenzo [3, 4] cyclohepta [1, 2-a] naphthalene derivatives as selective estrogen receptor modulators (SERMs) is described. The titled compounds were prepared in 9-21% overall yield with high chemical purity (> 97%) after nine consecutive synthetic steps.