TY - JOUR A1 - Gansäuer, Andreas A1 - Okkel, Andreas A1 - Schwach, Lukas A1 - Wagner, Laura A1 - Selig, Anja A1 - Prokop, Aram T1 - Triazol-substituted titanocenes by strain-driven 1,3-dipolar cycloadditions JF - Beilstein Journal of Organic Chemistry PY - 2014/// VL - 10 SP - 1630 EP - 1637 SN - 1860-5397 DO - 10.3762/bjoc.10.169 PB - Beilstein-Institut JA - Beilstein J. Org. Chem. UR - https://doi.org/10.3762/bjoc.10.169 KW - azides KW - click-chemistry KW - cycloadditions KW - cytotoxicity KW - titanocenes N2 - An operationally simple, convenient, and mild strategy for the synthesis of triazole-substituted titanocenes via strain-driven 1,3-dipolar cycloadditions between azide-functionalized titanocenes and cyclooctyne has been developed. It features the first synthesis of titanocenes containing azide groups. These compounds constitute ‘second-generation’ functionalized titanocene building blocks for further synthetic elaboration. Our synthesis is modular and large numbers of the complexes can in principle be prepared in short periods of time. Some of the triazole-substituted titanocenes display high cyctotoxic activity against BJAB cells. Comparison of the most active complexes allows the identification of structural features essential for biological activity. ER -