过渡金属介导的碳氢键后官能团化策略在药物合成中的研究进展

Recent advances in transition metal catalyzed late-stage C–H functionalization in medicinal chemistry

摘要:

过渡金属催化碳氢键后官能团化逐渐发展成为合成化学领域最有效的工具之一，是现代药物研发的重要组成部分，可以对生物活性分子进行高效且具有选择性地衍生。本文从C-C、C-O和C-N键三个方面对近十年来过渡金属参与催化具有生物活性的分子碳氢键后官能团化的研究进展简要概述，并对其局限性和未来发展趋势进行了总结和展望。

Abstract:

Transition metal catalyzed C–H bond direct activation has gradually developed as one of the most effective tools in synthetic chemistry and is an essential part of drug research and development, which can provide functionalized bioactive molecules in an efficient and selective fashion. The research progress of transition metal-catalyzed C–H bond late-stage functionalization of bioactive molecules in the past decade is summarized from three aspects: C–C, C–O and C–N bond formation. The limitations and future development are reviewed and prospected.