Versatile Methods for Palladium-Catalyzed Couplings

描述：(申请人描述)钯催化的偶联反应 是合成生物活性物质的非常有用的工具 化合物。我们建议为这些反应开发更强大的催化剂， 主要关注使用大体积、富电子的P(t-Bu)3作为 莱兰德。对于一系列重要的碳-碳键形成过程(例如， 铃木、Heck、Stille和Negishi联轴器)，我们打算开发： 有机氯化物偶联的一般方法.通用催化剂 在温和的条件下将有机溴化物、碘化物和三氟化物偶联(例如， 在室温下)以及有机磷酸盐和有机磷酸盐偶联的一般方法 对甲苯磺酸盐。 尽管我们的主要目标是提供实用的催化剂， 被合成化学家广泛应用于基础研究和 在药物/化学开发方面，我们还将进行机械学研究 旨在提供对不寻常起源的更好的理解 Pd/P(t-Bu)_3在这些偶联过程中的反应性。

DESCRIPTION: (Applicant's Description) Palladium-catalyzed coupling reactions serve as extremely useful tools for the synthesis of biologically active compounds. We propose to develop more powerful catalysts for these reactions, focusing primarily on complexes that employ bulky, electron-rich P(t-Bu)3 as a ligand. For an array of important carbon-carbon bond-forming processes (e.g., Suzuki, Heck, Stille, and Negishi couplings), we intend to develop: general methods for coupling organic chlorides; versatile catalysts for coupling organic bromides, iodides, and triflates under mild conditions (e.g., at room temperature) and general methods for coupling organic phosphates and tosylates. Although our primary objective is to provide practical catalysts that will be widely applied by synthetic chemists both in basic research and in pharmaceutical/chemical development, we will also pursue mechanistic studies directed at furnishing an improved understanding of the origin of the unusual reactivity of Pd/P(t-Bu)3 in these coupling processes.