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首页> 外文期刊>Polyhedron: The International Journal for Inorganic and Organometallic Chemistry >Towards peptide-substituted titanocene anticancer drugs
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Towards peptide-substituted titanocene anticancer drugs

机译：走向肽取代的钛茂抗癌药

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摘要

An alkyne-substituted fulvene was transformed via hydridolithiation followed by transmetallation with titanium tetrachloride into bis-[p-(prop-2-ynyloxy)-benzyl-cyclopentadienyl] titanium(IV) dichloride. Single crystals of this titanocene derivative could be obtained and the structure determined by X-ray diffraction. It showed that this compound crystallises in the space group C2/c with four molecules in the monoclinic cell. The alkyne-substituted titanocene dichloride derivative was then subject to a copper-catalysed azide-alkyne cycloaddition with its azide-functionalised methylester-protected phenylalanine reaction partner in order to form a linking triazole. This reaction was performed under anhydrous conditions employing a dichloromethane/acetonitrile solvent mixture with copper(I) iodide and 2,6-lutidine as the catalyst system. Under these conditions the adduct between the protein mimic and the titanocene was formed without hydrolysing the titanium dichloride moiety.
机译：炔烃取代的富勒烯经氢化锂化反应，然后与四氯化钛进行金属转移，转变为双-[对-（丙-2-炔氧基）-苄基-环戊二烯基]二氯化钛（IV）。可以得到该钛茂衍生物的单晶，并通过X射线衍射确定其结构。结果表明，该化合物在单斜细胞的C2 / c空间群中有四个分子结晶。然后将炔烃取代的二茂钛二氯化物衍生物与其叠氮化物官能化的甲基酯保护的苯丙氨酸反应伙伴进行铜催化的叠氮化物-炔烃环加成反应，以形成连接的三唑。该反应在无水条件下进行，使用二氯甲烷/乙腈溶剂混合物，其中碘化亚铜（I）和2，6-二甲基吡啶为催化剂体系。在这些条件下，在蛋白质模拟物和二茂钛之间形成了加合物，而没有水解二氯化钛部分。

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