Virtually instantaneous, room-temperature [(11)C]-cyanation using biaryl phosphine Pd(0) complexes.

Virtually instantaneous, room-temperature [(11)C]-cyanation using biaryl phosphine Pd(0) complexes.
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实际上,使用双磷蛋白PD(0)配合物,实际上是瞬时的,室温[(11)C]。

DOI:
10.1021/ja512115s
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发表时间:
2015-01-21
影响因子:
15
通讯作者:
Hooker, Jacob M.
Hooker, Jacob M.
中科院分区:
化学1区
文献类型:
--
作者:
Lee, Hong Geun;Milner, Phillip J.;Placzek, Michael S.;Buchwald, Stephen L.;Hooker, Jacob M.

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提出了一种新的放射合成[11 C]芳基腈的方法。该方法是基于原位合成的L·Pd(Ar)X配合物(L=联芳基膦)与[11 C]HCN的直接反应。该策略操作简单,表现出显着的宽底物范围与短的反应时间,并表现出上级的反应性相比,以前报道的系统。用这种方法,各种[11 C]腈类药物的制备具有高放射化学效率。
A new radiosynthetic protocol for the preparation of [11C]aryl nitriles has been developed. This process is based on the direct reaction of in situ prepared L•Pd(Ar)X complexes (L=biaryl phosphine) with [11C]HCN. The strategy is operationally simple, exhibits a remarkably wide substrate scope with short reaction times, and demonstrates superior reactivity compared to previously reported systems. With this procedure, a variety of [11C]nitrile-containing pharmaceuticals were prepared with high radiochemical efficiency.
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