An expedient route to substituted furans via olefin cross-metathesis
作者:Timothy J. Donohoe、John F. Bower
DOI:10.1073/pnas.0913466107
日期:2010.2.23
of highly substituted derivatives are essential to medicinal chemistry. Here we show that the olefin CM reaction, in combination with an acid cocatalyst or subsequent Heck arylation, provides a concise and flexible entry to 2,5-di- or 2,3,5-tri-substituted furans. These cascade processes portend further opportunities for the regiocontrolled preparation of other highly substituted aromatic and heteroaromatic
烯烃交叉复分解 (CM) 反应广泛用于有机化学,是选择性合成差异取代烯烃产物的有效方法。令人惊讶的是,尚未报道将这一非凡的过程整合到芳香族和杂芳香族构建策略中的努力。这种结构代表了大多数小分子药物化合物的关键要素;高度取代衍生物的受控制备方法对于药物化学是必不可少的。在这里,我们展示了烯烃 CM 反应与酸助催化剂或随后的 Heck 芳基化相结合,为 2,5-二-或 2,3,5-三-取代呋喃提供了简洁而灵活的入口。
SERIES OF SKIN-WHITENING (LIGHTENING) COMPOUNDS
申请人:Unigen, Inc.
公开号:EP2323612A1
公开(公告)日:2011-05-25
[EN] SERIES OF SKIN-WHITENING (LIGHTENING) COMPOUNDS<br/>[FR] FAMILLE DE COMPOSÉS PERMETTANT LE BLANCHIMENT (ÉCLAIRCISSEMENT) DE LA PEAU
申请人:UNIGEN PHARMACEUTICALS INC
公开号:WO2010011630A1
公开(公告)日:2010-01-28
The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.
Rate Enhanced Olefin Cross-Metathesis Reactions: The Copper Iodide Effect
作者:Karl Voigtritter、Subir Ghorai、Bruce H. Lipshutz
DOI:10.1021/jo200360s
日期:2011.6.3
Copper iodide has been shown to be an effective cocatalyst for the olefin cross-metathesis reaction. In particular, it has both a catalyst stabilizing effect due to iodide ion, as well as copper(I)-based phosphine-scavenging properties that apply to use of the Grubbs-2 catalyst. A variety of Michael acceptors and olefinic partners can be cross-coupled under mild conditions in refluxing diethyl ether