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.

  • 01 March 2024   News

    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.

  • 21 February 2024   Press Release

    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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Advanced Synthesis and Catalysis 2020, 362 (15), 3229-3242

DOI: 10.1002/adsc.202000450

Tereshchenko O.; Perebiynis M.; Knysh I.; Vasylets O.; Sorochenko A.; Slobodyanyuk E.; Rusanov E.; Borysov O.; Kolotilov S.; Ryabukhin S.; Volochnyuk D.

The electrochemical Shono oxidation of Boc-protected cyclic amines was revised. The conditions for scalable electrochemical synthesis of cyclic enecarbamates were found. The developed protocol included recycling of the full range of used reagents, favoring to E-factor reduction according to Green Chemistry requirements. The method opened the way for the convenient preparation of previously uncommon materials, which could become useful synthetic intermediates. Their synthetic potential was evaluated in [2+1] and [2+2] cycloadditions as well as electrophilic functionalization. Moreover, functionalized enecarbamates with carbonyl groups in β-position were used as latent 1,3-bielectrophiles in classical heterocyclizations. In a case of the hydrazine, the corresponding unusually decorated pyrazoles were prepared. The proposed methodology is a straightforward tool for the design and synthesis of Medicinal Chemistry relevant building blocks. As examples, 5-fluoro pipecolic and 3-fluoro isonipecotic acids were synthesized starting from Boc-protected esters of the pipecolic and the isonipecotic acids respectively; the 5-step approach to pyrazole containing α-aminoacids with different linkers between the aminoacidic and pyrazole moieties was elaborated based on the cheapest commercially available racemic and chiral cyclic α-aminoacids; the convenient approach to the functionalized tetrahydropyrido[3,4-d]pyridazines was proposed starting from Boc-protected ester of the isonipecotic acids.

Electrochemical Scaled-up Synthesis of Cyclic Enecarbamates as Starting Materials for Medicinal Chemistry Relevant Building Bocks

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