1755-45-9Relevant articles and documents
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors
Albrecht, Brian K.,Audia, James E.,Balasubramanian, Srividya,Bellon, Steven F.,Brucelle, Francois,Cummings, Richard T.,Duplessis, Martin,Gehling, Victor S.,Good, Andrew C.,Harmange, Jean-Christophe,Iyer, Priyadarshini,Khanna, Avinash,Levell, Julian R.,McGrath, John P.,Sawant, Priyanka,Stuckey, Jacob,Trojer, Patrick,Vaswani, Rishi G.,Watson, Venita,C?té, Alexandre
, p. 1213 - 1220 (2020)
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the FAD cofactor of LSD1.
Binuclear Pd(I)-Pd(I) Catalysis Assisted by Iodide Ligands for Selective Hydroformylation of Alkenes and Alkynes
Zhang, Yang,Torker, Sebastian,Sigrist, Michel,Bregovi?, Nikola,Dydio, Pawe?
supporting information, p. 18251 - 18265 (2020/11/02)
Since its discovery in 1938, hydroformylation has been thoroughly investigated and broadly applied in industry (>107 metric ton yearly). However, the ability to precisely control its regioselectivity with well-established Rh- or Co-catalysts has thus far proven elusive, thereby limiting access to many synthetically valuable aldehydes. Pd-catalysts represent an appealing alternative, yet their use remains sparse due to undesired side-processes. Here, we report a highly selective and exceptionally active catalyst system that is driven by a novel activation strategy and features a unique Pd(I)-Pd(I) mechanism, involving an iodide-assisted binuclear step to release the product. This method enables β-selective hydroformylation of a large range of alkenes and alkynes, including sensitive starting materials. Its utility is demonstrated in the synthesis of antiobesity drug Rimonabant and anti-HIV agent PNU-32945. In a broader context, the new mechanistic understanding enables the development of other carbonylation reactions of high importance to chemical industry.
INHIBITORS OF METALLO-BETA-LACTAMASES
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Paragraph 00225; 00226, (2018/12/13)
The present invention relates to compounds of Formula (I) that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection. (Formula (I))