期刊
ACS COMBINATORIAL SCIENCE
卷 13, 期 5, 页码 501-510出版社
AMER CHEMICAL SOC
DOI: 10.1021/co200090p
关键词
parallel synthesis; desketoraloxifene; iodocyclization; benzo[b]thiophene; selective estrogen receptor modulator (SERM); palladium coupling
资金
- National Institute of General Medical Sciences [GM070620, GM079593]
- National Institutes of Health Kansas University Chemical Methodologies and Library Development Center of Excellence [GM069663]
For a future structure-activity relationship (SAR) study, a library of desketoraloxifene analogues has been prepared by parallel synthesis using iodocyclization and subsequent palladium-catalyzed coupling reactions. Points of desketoraloxifene diversification involve the two phenolic hydroxyl groups and the aliphatic amine side chain. This approach affords oxygen bearing 3-iodobenzo[b]thiophenes 4 in excellent yields, which are easily further elaborated using a two-step approach involving Suzuki-Miyaura and Mitsunobu coupling reactions to give multimethoxy-substituted desketoraloxifene analogues 6. Various hydroxyl-substituted desketoraloxifene analogues 7 were subsequently generated by demethylation with BBr(3).
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据