From Process Chemistry to Methodology Development in Metal-Mediated Chemistry and Catalysis
金属介导化学和催化在改变我们开发化学反应的方式方面发挥着关键作用，为生产必需化合物提供了更环保、更高效的途径。在本期Thieme有机化学研讨会中，我们将探索从工艺化学到创新方法的历程，并了解这些强大的工具如何加速整个领域的突破！
本次活动将由SYNTHESIS、 SYNFACTS编辑、德国柏林工业大学 (TU) 的Martin Oestreich教授主持。来自德国图宾根大学的Ivana Fleischer教授、西班牙Eurofins Villapharma Research的Matthew Horwitz教授以及意大利都灵大学的Vittorio Pace教授将分享他们的研究。
1. Catalysis and C–S bonds
Ivana Fleischer
University of Tuebingen, Germany
Our research interests focus on development of new methods for the synthesis and use of sulfur-containing compounds, such as thioesters and thioethers. They constitute valuable synthetic intermediates and target compounds for material chemistry and pharmaceutical applications. Our aim is to develop efficient transformations employing non-precious metals as homogeneous catalysts. We have demonstrated the usefulness of thioesters in cross coupling reactions with arylzinc reagents to generate ketones. A defined nickel complex was employed as catalyst and a series of functionalized ketones was successfully obtained. The scope was later expanded to the coupling of thioesters with more reactive organomanganese reagents upon iron catalysis. Furthermore, we developed nickel-catalyzed coupling reactions of challenging aryl chlorides with thiols, whereby max. TOF of 800 h-1 was achieved. A broad scope of substrates containing various functional groups and heterocyclic motifs was successfully converted. Further systematic studies of couplings of sterically hindered aliphatic thiols with a broad range of electrophiles, including ortho-substituted triflates, were conducted.2. What is Discovery Process Chemistry? Introduction and State of the Art
Matthew Horwitz
Eurofins Villapharma Research, Spain
Discovery Process Chemistry (DPC) is an emerging intersectoral space that is characterized by the development of new chemical reactions or syntheses that enable the efficient elucidation of structure-activity relationships (SARs) and structure-property relationships (SPRs) as well as a rapid transition to process development. Drug discovery and development are accelerated by such efforts and this has led chemists in academia and industry alike to place an increasing importance on these aims. In this seminar, we explore recent advances in DPC and the impact that it can have on SAR/SPR interrogation and downstream drug development efforts.3. Designing New Synthetic Concepts for Imparting Molecular Complexity with C-1 Sources
Vittorio Pace
University of Turin, Italy
The direct transfer of a reactive nucleophilic CH2X unit into an existing linkage enables the formal introduction of the moiety with the precisely defined degree of functionalization. Upon the fine tuning of the reaction conditions governing the transformation, the initial homologation event can serve as the manifold for triggering unusual rearrangement sequences leading to complex architectures through a unique synthetic operation. The direct – full chemoselective - conversion of a ketone into the homologated all-carbon quaternary aldehyde (via a), the telescoped homologation of imine-surrogates to quaternary aziridines (via b) and bis-trifluoromethyl-β-diketiminates (via c) will illustrate these unprecedented concepts. Additionally, the homologation of disulfides and thiosulfonates will furnish symmetrical (via d) and unsymmetrical oxothio- and dithio-acetals (via e). The one-step mono-fluoromethylation of carbon electrophiles with extremely labile fluoromethyllithium reagents will provide a novel entry to valuable fluorinated building-blocks without the needing of using protecting elements for fluoro-containing carbanions (via f). Finally, the development of homologation strategies not relying on the use of external C1-sources will be discussed.声明：此文是出于传递更多信息之目的。部分图片、资料来源于网络，版权归原作者所有，如有侵权请联系后台删除。
