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11 April 2024
Press Release
Cambridge, UK and Kyiv, Ukraine, 11 April 2024: Metrion Biosciences Limited (“Metrion”), the specialist ion channel and cardiac safety screening contract research organisation (CRO) and drug discovery company, and Enamine Ltd (“Enamine”), the global leader in supplying small molecules and early drug discovery services, announced that Metrion has enhanced its High Throughput Screening (HTS) services with the addition of access to Enamine’s compound libraries.
27 March 2024
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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.
J. Org. Chem.
2020, 85 (4), 2321-2337
DOI:
10.1021/acs.joc.9b03044
Semeno V.; Vasylchenko V.; Vashchenko B.; Lutsenko D.; Iminov R.; Volovenko O.; Grygorenko O.
An approach to 1,3-disubstitued bicyclo[2.1.0]pentane (housane) derivatives was developed. The method relied on lithium bis(trimethylsilyl)amide-mediated intramolecular cyclization of trisubstitued cyclopentane carboxylates bearing a leaving group (at the C-4 position) and an additional substituent (at the C-3 atom), in turn synthesized from cyclopent-3-ene carboxylate. The synthetic sequence allowed for the preparation of both cis- and trans-1,3-disubstituted housane-1-carboxylic acids in diastereoselective manner on up to 80 g scale. In particular, bicyclic γ-amino acids—γ-aminobutyric acid analogues—were synthesized. It was shown that the bicyclo[2.1.0]pentane did not significantly affect pKa of the corresponding derivatives and slightly increased their hydrophilicity (by 0.07–0.25 LogP units) as compared to cyclopentane. X-ray diffraction studies showed that cis- and trans-1,3-disubstituted housanes can be considered as flattened analogues of the corresponding cyclopentane derivatives with fixed envelope conformation of the five-membered ring.
![Building the Housane: Diastereoselective Synthesis and Characterization of Bicyclo[2.1.0]pentane Carboxylic Acids](/images/publications/2019/101021-acsjoc9b03044.png)
