Roslin Sara, Odell Luke R
Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala Biomedical Center, Uppsala University, P. O. Box 574, SE-751 23, Uppsala, Sweden.
Chem Commun (Camb). 2017 Jun 22;53(51):6895-6898. doi: 10.1039/c7cc02763j.
Herein, a simple and efficient method for the palladium-catalyzed carbonylation of aryl boronic acids with unactivated alkyl iodides and bromides under visible-light irradiation, ambient temperature and low CO-pressure is presented. Notably, the procedure uses readily available equipment and an inexpensive palladium catalyst to generate the key alkyl radical intermediate. These mild conditions enabled the synthesis of a range of functionalized aryl alkyl ketones including the antipsychotic drug, melperone.
在此,我们报道了一种简单高效的方法,即在可见光照射、室温及低一氧化碳压力下,钯催化芳基硼酸与未活化的烷基碘化物和溴化物进行羰基化反应。值得注意的是,该方法使用易于获得的设备和廉价的钯催化剂来生成关键的烷基自由基中间体。这些温和的条件使得一系列功能化芳基烷基酮得以合成,包括抗精神病药物美哌隆。