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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
27 March 2024
Press Release
March, 2024, Kyiv, Ukraine. Enamine Ltd, the global leader in supplying small molecules and early drug discovery services, announces the expansion of its library synthesis capabilities with a focus on Enamine REAL compounds to further support the growing demands of agricultural and pharmaceutical companies, research institutes, and drug discovery centers.
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.
Eur. J. Org. Chem.
2021, 2021 (47), 6530‑6540
DOI:
10.1002/ejoc.202000351
Stepannikova K.; Vashchenko B.; Grygorenko O.; Gorichko M.; Cherepakha A.; Moroz Y.; Volovenko Y.; Zhersh S.
One‐pot intramolecular cyclization of novel sp3‐enriched cyanoalkylsulfonyl fluorides into spirocyclic β‐ or γ‐sultams is disclosed. The method relies on nitrile group reduction followed by sulfonylation of amino group thus formed upon mild conditions (NaBH4, NiCl2⋅6H2 O in MeOH). Cyclization proceeds smoothly with considerable efficiency (58–85%, 10 examples) on up to 30 g scale. The cyanoalkylsulfonyl fluoride intermediates can be obtained via S‐nucleophilic substitution in β‐functionalized alkanenitriles or double alkylation of α‐alkylthioacetonitrile, followed by oxidative chlorination with Cl2 and further reaction with KHF2. The title mono‐ and bifunctional sultams are advanced sp3‐enriched building blocks for drug discovery and organic synthesis providing novel substitution patterns and frameworks mimicking saturated nitrogen heterocycles such as pyrrolidine/pyrrolidone.