Departamento de Química Inorgánica, Instituto de Síntesis Química y Catálisis Homogénea (ISQCH), Universidad de Zaragoza-CSIC, E-50009 Zaragoza, Spain.
Dalton Trans. 2015 May 21;44(19):9052-62. doi: 10.1039/c5dt00703h.
A new amine gold(III) complex [Au(C6F5)2(DPA)]ClO4 with the di-(2-picolyl)amine (DPA) ligand has been synthesised. In the solid state the complex has a chiral amine nitrogen because the ligand coordinates to the gold centre through one nitrogen atom from a pyridine and through the NH moiety, whereas in solution it shows a fluxional behaviour with a rapid exchange between the pyridine sites. This complex can be used as an excellent synton to prepare new gold(III) carbene complexes by the reaction with isocyanide CNR. The resulting gold(III) derivatives have unprecedented bidentate C^N acyclic carbene ligands. All the complexes have been spectroscopically and structurally characterized. Taking advantage of the fluxional behaviour of the amine complex, its catalytic properties have been tested in several reactions with the formation of C-C and C-N bonds. The complex showed excellent activity with total conversion, without the presence of a co-catalyst, and with a catalyst loading as low as 0.1%. These complexes also present biological properties, and cytotoxicity studies have been performed in vitro against three tumour human cell lines, Jurkat (T-cell leukaemia), MiaPaca2 (pancreatic carcinoma) and A549 (lung carcinoma). Some of them showed excellent cytotoxic activity compared with the reference cisplatin.
一种新型的胺金（III）配合物[Au（C6F5）2（DPA）]ClO4与二（2-吡啶基）胺（DPA）配体已被合成。在固态下，该配合物具有手性胺氮，因为配体通过吡啶的一个氮原子和 NH 部分与金中心配位，而在溶液中，它表现出快速的吡啶交换行为。这种配合物可以用作一个极好的合成子，通过与异氰化物 CNR 反应来制备新的金（III）卡宾配合物。所得的金（III）衍生物具有前所未有的双齿 C^N 非环卡宾配体。所有的配合物都进行了光谱和结构表征。利用胺配合物的动态行为，对其在几种 C-C 和 C-N 键形成反应中的催化性能进行了测试。该配合物在没有共催化剂的情况下，以低至 0.1%的催化剂负载量，表现出优异的活性和完全转化。这些配合物还具有生物特性，并在体外对三种人类肿瘤细胞系 Jurkat（T 细胞白血病）、MiaPaca2（胰腺癌）和 A549（肺癌）进行了细胞毒性研究。与参考顺铂相比，其中一些表现出优异的细胞毒性活性。
