Koolma Victor, Staiger Roman, Schühle Martin, Bixenmann Achim, Bauschatz Elmar, Schmid Matthias, Miloserdov Fedor M, Herlé Bart
Boehringer Ingelheim Pharma GmbH & Co. KG, 88400, Biberach an der Riss, Germany.
Laboratory of Organic Chemistry, Wageningen University, Stippeneng 4, 6708 WE Wageningen, The Netherlands.
Org Lett. 2024 Apr 12;26(14):2852-2856. doi: 10.1021/acs.orglett.3c03873. Epub 2023 Dec 15.
General and robust conditions for the Liebeskind-Srogl coupling were developed and used in functionalization of medicinal-chemistry-relevant heterocyclic substrates. Applicability in HTE and library synthesis, combined with its orthogonality to other cross-coupling reactions, make it highly attractive for discovery chemistry workflows. Additionally, the results suggest that the nature of the Cu(I)-carboxylate plays a more prominent role in the reaction performance than the nature of Pd-catalysts, which is rather uncommon for Pd-catalysis and can be used in further optimization of Liebeskind-Srogl coupling.
已开发出适用于利伯斯金德-施罗格偶联反应的通用且稳健的条件，并将其用于与药物化学相关的杂环底物的官能化反应中。该反应在高通量实验（HTE）和库合成中的适用性，以及与其他交叉偶联反应的正交性，使其在发现化学工作流程中极具吸引力。此外，结果表明，与钯催化剂的性质相比，羧酸铜（I）的性质在反应性能中起着更突出的作用，这在钯催化中相当罕见，可用于进一步优化利伯斯金德-施罗格偶联反应。
