Building Blocks Catalog

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Building Blocks

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2 000 new building blocks are synthesized monthly. Here is an important update to our MedChem Highlights from February 2024

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  • 27 March 2024   Press Release

    Enamine Announces Expansion of Its Library Synthesis Capabilities

    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.

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    Enamine and Genez International Announce Strategic Collaboration to Launch ...

    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.

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    Cresset Announces Global Collaboration With Enamine on New Virtual ...

    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.

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Eur. J. Org. Chem. 2019 (22), 3636-3648

DOI: 10.1002/ejoc.201900450

Subota A.; Lutsenko A.; Vashchenko B.; Volochnyuk D.; Levchenko V.; Dmytriv Y.; Rusanov E.; Gorlova A.; Ryabukhin S.; Grygorenko O.

An efficient approach towards introducing (cyclo)alkyl substituents at C‐2, C‐3 or C‐4 positions of the piperidine ring was described. The method relied on the straightforward two‐step reaction sequence based on the formal sp3–sp3 retrosynthetic disconnection. The procedure commenced with selective directed ortho metalation of 2‐ and 3‐bromopyridine, followed by reaction with aldehydes or ketones. The optimized methods were developed for all three isomers of hydroxyalkyl‐substituted pyridines, which were synthesized in 28–84 % overall yield (20 examples). Catalytic hydrogenation of these adducts could be performed selectively with or without retention of the hydroxyl group in their molecules, so that either (cyclo)alkylpiperidines (14 examples) or the corresponding saturated amino alcohols (16 examples) were obtained (28–96 % and 82–96 % yield, respectively). After minor modifications, the developed method was also implemented in a flow reactor and a 5 L autoclave, which allowed for the preparation of up to 0.5 kg of the representative (cyclo)alkylpiperidines.

Scalable and Straightforward Synthesis of All Isomeric (Cyclo)alkylpiperidines

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