Lim Daniel, Fang Fang, Zhou Guoqiang, Coltart Don M
Department of Chemistry, Duke University, Durham, North Carolina 27708, USA.
Org Lett. 2007 Oct 11;9(21):4139-42. doi: 10.1021/ol701599v. Epub 2007 Sep 18.
Ketones undergo soft enolate formation and acylation on treatment with MgBr(2).OEt(2), i-Pr(2)NEt, and various acylating agents to give 1,3-diketones. The process is particularly efficient for N-acylbenzotriazoles and O-Pfp esters, and, in these cases, is conducted with untreated, reagent-grade CH(2)Cl(2) open to the air, thus providing an exceptionally simple approach to the synthesis of this important class of compounds.
酮类化合物在与MgBr₂·OEt₂、二异丙基乙胺(i-Pr₂NEt)及各种酰化剂反应时,会发生烯醇盐的温和生成及酰化反应,生成1,3 - 二酮。该过程对于N - 酰基苯并三唑和O - 五氟苯基酯尤为有效,在这些情况下,反应在未处理的、试剂级且敞口于空气中的二氯甲烷(CH₂Cl₂)中进行,从而为合成这类重要化合物提供了一种极其简便的方法。