Cohen Daniel T, Buchwald Stephen L
Department of Chemistry, Massachusetts Institute of Technology , Cambridge, Massachusetts 02139, United States.
Org Lett. 2015 Jan 16;17(2):202-5. doi: 10.1021/ol5032359. Epub 2015 Jan 2.
A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 2-5 mol % catalyst loadings with temperatures ranging from rt to 40 °C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.
报道了一种温和、高效且低温的钯催化（杂）芳基卤化物和三氟甲磺酸酯的氰化反应。以往钯催化的（杂）芳基卤化物氰化反应需要更高的温度才能实现良好的催化活性。当前的反应能够在2 - 5 mol%的催化剂负载量以及室温至40℃的温度范围内，对多种（杂）芳基卤化物和三氟甲磺酸酯进行氰化反应。这种温和的方法被应用于逆转录酶抑制剂lerivirine的合成。
