Building Blocks Catalog

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Building Blocks

1B novel building blocks

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

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  • 11 April 2024   Press Release

    Metrion Biosciences enhances High Throughput Screening services with access ...

    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   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.

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Tetrahedron , 2011, 67 (34), 6233-6239

DOI: 10.1016/j.tet.2011.06.063

Cherepakha A.; Kovtunenko V. O.; Tolmachev A.; Lukin O.

Condensations of o-halo-substituted benzenesulfonyl chlorides with 2-aminopyridines and amidines may give the corresponding 1,2,4-benzothiadiazine-1,1-dioxides under mild, non-catalytic conditions in nearly quantitative yields. The successful one-pot cyclization depends on three factors: (i) the nature of the o-halogen, (ii) the electronic character of the benzene ring substituent, and (iii) the steric load around the amidine unit. O-Fluorobenzenesulfonyl chlorides bearing methylcarboxyl- or nitro-group and o-chloro- and o-bromobenzenesulfonyl chlorides bearing nitro-group are reactive enough to give the desired 1,2,4-benzothiadiazine-1,1-dioxides in a one-pot base-promoted reaction. In all other cases, open-chain sulfonylated amidine intermediates are isolated. The latter are converted to the title compounds either in the presence of potassium carbonate or upon the addition of a copper(I) catalyst.

A one-pot, non-catalytic approach to 1,2,4-benzothiadiazine-1,1-dioxides

Cherepakha A.; Kovtunenko V. O.; Tolmachev A.; Lukin O.
Tetrahedron 2011, 67 (34), 6233-6239
DOI: 10.1016/j.tet.2011.06.063

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