Compounds Currently in Phase II−III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas Yu Zhou,† Jiang Wang,† Zhanni Gu,† Shuni Wang,† Wei Zhu,† Jose ́ Luis Aceña,*,‡,§ Vadim A. Soloshonok,*,‡,∥ Kunisuke Izawa,* and Hong Liu*,† †Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China ‡Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizab́al 3, 20018 San Sebastiań, Spain Department of Organic Chemistry, Autońoma University of Madrid, Cantoblanco, 28049 Madrid, Spain IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, 48013 Bilbao, Spain Hamari Chemicals Ltd., 1-4-29 Kunijima, Higashi-Yodogawa-ku, Osaka, Japan 533-0024

Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas

Over the past decade, the most significant, conceptual advances in the field of fluorination were enabled most prominently by organo- and transition-metal catalysis. The most challenging transformation remains the formation of the parent C-F bond, primarily as a consequence of the high hydration energy of fluoride, strong metal-fluorine bonds, and highly polarized bonds to fluorine. Most fluorination reactions still lack generality, predictability, and cost-efficiency. Despite all current limitations, modern fluorination methods have made fluorinated molecules more readily available than ever before and have begun to have an impact on research areas that do not require large amounts of material, such as drug discovery and positron emission tomography. This Review gives a brief summary of conventional fluorination reactions, including those reactions that introduce fluorinated functional groups, and focuses on modern developments in the field.

/pdf/introduction-of-fluorine-and-fluorine-containing-functional-1i8kwiad20.pdf

Introduction of Fluorine and Fluorine-Containing Functional Groups

Flow chemistry involves the use of channels or tubing to conduct a reaction in a continuous stream rather than in a flask Flow equipment provides chemists with unique control over reaction parameters enhancing reactivity or in some cases enabling new reactions This relatively young technology has received a remarkable amount of attention in the past decade with many reports on what can be done in flow Until recently, however, the question, “Should we do this in flow?” has merely been an afterthought This review introduces readers to the basic principles and fundamentals of flow chemistry and critically discusses recent flow chemistry accounts

The Hitchhiker's Guide to Flow Chemistry

Catalytic Enantioselective Addition of Allylic Organometallic Reagents to Aldehydes and Ketones

Good Partnership between Sulfur and Fluorine: Sulfur-Based Fluorination and Fluoroalkylation Reagents for Organic Synthesis

Chiral titanium complexes for enantioselective addition of nucleophiles to carbonyl groups

Fluorine containing organic agents play a crucial role in the search for new active pharmaceutical and agrochemical compounds. Owing to their fluorine moieties, these compounds have unique chemical and physical properties. For example, they can increase the metabolic stability or the lipophilicity, which can enhance the biological activity of a drug. For these reasons, the CF3 group is an essential moiety of numerous commercially available aromatic and non-aromatic biological active agents. Therefore, the research on new

Ortho-trifluoromethylation of functionalized aromatic triazenes.

The ability to form multiple carbon-carbon bonds in a controlled sequence and thus rapidly build molecular complexity in an iterative fashion is an important goal in modern chemical synthesis. In recent times, transition-metal-catalysed coupling reactions have dominated in the development of C-C bond forming processes. A desire to reduce the reliance on precious metals and a need to obtain products with very low levels of metal impurities has brought a renewed focus on metal-free coupling processes. Here, we report the in situ preparation of reactive allylic and benzylic boronic acids, obtained by reacting flow-generated diazo compounds with boronic acids, and their application in controlled iterative C-C bond forming reactions is described. Thus far we have shown the formation of up to three C-C bonds in a sequence including the final trapping of a reactive boronic acid species with an aldehyde to generate a range of new chemical structures.

/pdf/iterative-reactions-of-transient-boronic-acids-enable-l4jxi5id7u.pdf

Iterative reactions of transient boronic acids enable sequential C–C bond formation

The {sup 53}Cr NMR spectra of 46 chromium-carbene complexes were recorded, and chemical shift and line width data are reported, along with associated infrared, uv-visible, and {sup 13}C NMR spectroscopic data. The {sup 53}Cr chemical shifts correlated very well with the donor-acceptor properties of the carbene ligand and were quite sensitive to steric influences on efficiency of {pi}-overlap of the heteroatom with the carbene carbon. There was no correlation of {delta}({sup 53}Cr) with reactivity toward imines to form {beta}-lactams, but line width appeared to be related to reactivity. Preliminary attempts to utilize {sup 53}Cr NMR data to direct synthetic utilization of chromium-carbene complexes are reported. 5 refs., 49 figs., 1 tab.

Chromium-53 nuclear magnetic resonance studies of pentacarbonylchromium carbene complexes

Photoinduced Ring‐Opening Metathesis Polymerization (PROMP) with Photochemically Generated Schrock‐Type Catalysts

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