Synthesis of Tetracyclic Heterocompounds as Selective Estrogen Receptor Modulators. Part 1. Process Development for Scale-up of 2,5,8-Substituted 5,11-Dihydrochromeno[4,3-c]chromene Derivatives
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- 作者：Xun Li ; Michael Reuman ; Ronald K. Russell ; Richard Adams ; Robert Ma ; Sandra Beish ; Shawn Branum ; Scott Youells ; Jerry Roberts ; Nareshkumar Jain ; Ramesh Kanojia ; Zhihua Sui
- 刊名：Organic Process Research & Development
- 出版年：2007
- 出版时间：May 2007
- 年：2007
- 卷：11
- 期：3
- 页码：414 - 421
- 全文大小：114K
- 年卷期：v.11,no.3(May 2007)
- ISSN：1520-586X
文摘
Unsymmetrical benzopyranobenzopyran compounds are novelselective estrogen receptor modulators (SERMs). A reproducibleand nonchromatographic process was developed to preparemultihundred gram quantities of 5-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-5,11-dihydrochromeno[4,3-c]chromene-2,8-diyl-bis(2,2-dimethylpropanoate) (14). The overall yield of this 11-stepsynthesis was improved from 0.17% to 7.1% after three scale-up campaigns.