Department of Chemistry , University of Michigan , 930 North University Avenue , Ann Arbor , Michigan 48109 , United States.
Department of Radiology , University of Michigan Medical School , 1301 Catherine Street , Ann Arbor , Michigan 48109 , United States.
Org Lett. 2018 Mar 16;20(6):1530-1533. doi: 10.1021/acs.orglett.8b00242. Epub 2018 Feb 27.
A copper-mediated method for the transformation of diverse arylboron compounds and arylstannanes to aryl-[C]-nitriles is reported. This method is operationally simple, uses commercially available reagents, and is compatible with a wide variety of substituted aryl- and heteroaryl substrates. This method is applied to the automated synthesis of high specific activity [C]perampanel in 10% nondecay-corrected radiochemical yield (RCY).
本文报道了一种铜介导的方法，可将各种芳基硼酸化合物和芳基锡烷转化为芳基-[C]-腈。该方法操作简单，使用商业上可获得的试剂，并且与各种取代的芳基和杂芳基底物兼容。该方法应用于[C]培高利特的全自动合成，非衰变校正的放射性化学产率（RCY）为 10%。
