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2 000 new building blocks are synthesized monthly. Here is an important update to our MedChem Highlights from February 2024
Recent News
01 March 2024
News
We are excited to announce a strategic collaboration between Enamine, the world's leading provider of chemical building blocks, compound libraries, and biology services, and Genez International, a prominent enterprise with 15 years of experience in cross-border supply management, biopharmaceutical research and development, semiconductor equipment, and high-definition digital imaging systems.
21 February 2024
Press Release
Cresset recently announced a collaboration with Enamine, the world’s leading provider of chemical building blocks and drug discovery services to develop innovative new solutions for the early drug discovery process.
11 January 2024
Press Release
SyntheticGestalt, a research and development company specializing in the application of AI to the life sciences domain, and Enamine, the world’s leading provider of chemical building blocks, screening compounds, and integrated drug discovery services, have announced the start of a joint effort to create a suite of AI models that will enable the generation of synthetically accessible biologically active compounds with optimized physicochemical and ADME/ Tox properties. The models will be applicable to the compound discovery initiatives of SyntheticGestalt, as well as its service for both academic users and pharmaceutical companies.
J. Org. Chem.
2021, 86 (11), 7315-7325
DOI:
10.1021/acs.joc.0c03038
Sotnik S.; Subota A.; Kliuchynskyi A.; Yehorov D.; Lytvynenko A.; Rozhenko A.; Kolotilov S.; Ryabukhin S.; Volochnyuk D.
A Cu-catalyzed, easily scalable one-pot synthesis of fused pyridines by the reaction of cyclic ketones with propargylamine is described. The protocol was optimized based on the results of more than 30 experiments. The highest product yields were achieved in i-PrOH as a solvent in the presence of 5.0 mol % CuCl2 in air. In contrast to the well-known Au-catalyzed protocol, our procedure is “laboratory friendly”, cost-effective, and suitable for preparing dozens of grams of fused pyridine-based building blocks and does not require a high-pressure autoclave technique. Decreasing the catalyst amount in the reaction to 1.25 mol % CuCl2 provided a yield comparable to that achieved with 5 mol % catalyst, though a longer reaction time was required. A plausible reaction mechanism was proposed. The scope and limitation of the reaction were studied using 24 different cyclic ketones as starting materials. The fused pyridine yield decreased among cyclic ketones in the following order: six-membered ≫ eight-membered > five-membered ∼ seven-membered. The elaborated reaction conditions demonstrated tolerance to a number of protective functional groups in ketone such as ester, tert-butoxycarbonyl (Boc)-protected amine, and acetal moieties.