Versatile Methods for Palladium-Catalyzed Couplings

描述：（申请人的描述）钯催化的偶联反应 作为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， 主要集中在配合物，采用庞大的，富电子的P（t-Bu）3作为一个 配体。对于一系列重要的碳-碳键形成过程（例如， Suzuki、Heck、Stille和Negishi联轴器），我们打算开发： 偶联有机氯化物的一般方法.多用途催化剂 在温和条件下偶联有机溴化物、碘化物和三氟甲磺酸酯（例如， 在室温下）和偶联有机磷酸酯和 甲苯磺酸盐。 虽然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 药物/化学开发，我们还将进行机理研究 旨在加深对不寻常的起源的理解 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.