A Palladium-Catalyzed Double Carbonylation Approach to Isatins from 2-Iodoanilines
作者:Simon R. Laursen、Mikkel T. Jensen、Anders T. Lindhardt、Mikkel F. Jacobsen、Troels Skrydstrup
DOI:10.1002/ejoc.201600143
日期:2016.4
A high-yielding procedure for the synthesis of isatins has been developed. Sequential Pd-catalyzed double carbonylation of 2-iodoanilines with near stoichiometric amounts of CO followed by acid-promoted cyclization readily affords an array of isatins. The conversion of 2-iodoanilines to isatins in good to excellent yields was found to proceed with good functional group tolerance. This protocol proved
已开发出合成靛红的高产程序。用接近化学计量的 CO 对 2-碘苯胺进行连续 Pd 催化双羰基化,然后进行酸促进环化,很容易得到一系列靛红。发现 2-碘苯胺以良好到极好的产率转化为靛红,具有良好的官能团耐受性。该协议证明适用于靛红的 13C 同位素标记, 并扩展到 13C 同位素标记的抗病毒药物美替沙宗和实验性抗精神分裂症药物 ML137 的合成。