1152582-56-3Relevant academic research and scientific papers
Synthesis of 1-hetaryl-2,2-difluorocyclopropane-derived building blocks: The case of pyrazoles
Nosik, Pavel S.,Ryabukhin, Sergey V.,Pashko, Mykola O.,Grabchuk, Galyna P.,Grygorenko, Oleksandr O.,Volochnyuk, Dmitriy M.
, p. 80 - 89 (2019)
An approach to 1-hetaryl-2,2-difluorocyclopropane building blocks compatible with the current criteria of lead-oriented synthesis was developed and implemented for the case of 3-, 4- and 5-subsituted pyrazole derivatives. The method implied 6–9 synthetic steps, including difluorocyclopropanation with the TMSCF3–NaI system as the key transformation, and provided the title compounds on up to gram scale. The scope of the procedures towards substitution in the pyrazole ring and typical functional groups (i.e. COOH, NH2, CH2NH2, CH2OH) was established. The results obtained allowed formulation of preliminary guidelines for the synthetic feasibility of various functionalized 1-hetaryl-2,2-difluorocyclopropanes. 2018 Elsevier Ltd. All rights reserved.
Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α
Buckley, Dennis L.,Gustafson, Jeffrey L.,Van-Molle, Inge,Roth, Anke G.,Tae, Hyun Seop,Gareiss, Peter C.,Jorgensen, William L.,Ciulli, Alessio,Crews, Craig M.
supporting information, p. 11463 - 11467 (2013/01/15)
By design: Novel small-molecule inhibitors of the interaction between the von Hippel-Lindau ligase (VHL) and its molecular target HIF1α, a transcription factor involved in oxygen sensing, have been developed and studied. The most potent inhibitor binds with an IC50 value of 0.9-μM and is thus the first sub-micromolar inhibitor of the VHL-HIF1α interaction. Copyright
