{"id":2422,"date":"2018-11-19T11:23:45","date_gmt":"2018-11-19T11:23:45","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/journal-paper\/combining-two-directional-synthesis-and-tandem-reactions-part-21-exploitation-of-a-dimeric-macrocycle-for-chain-terminus-differentiation-and-synthesis-of-an-sp3-rich-library\/"},"modified":"2018-11-19T11:23:45","modified_gmt":"2018-11-19T11:23:45","slug":"combining-two-directional-synthesis-and-tandem-reactions-part-21-exploitation-of-a-dimeric-macrocycle-for-chain-terminus-differentiation-and-synthesis-of-an-sp3-rich-library","status":"publish","type":"journal-paper","link":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/combining-two-directional-synthesis-and-tandem-reactions-part-21-exploitation-of-a-dimeric-macrocycle-for-chain-terminus-differentiation-and-synthesis-of-an-sp3-rich-library\/","title":{"rendered":"Combining two-directional synthesis and tandem reactions – Part 21: Exploitation of a dimeric macrocycle for chain terminus differentiation and synthesis of an sp3-rich library"},"content":{"rendered":"

Thomas E .Storra, Sarah J. Cully, Michael J. Rawling, William Lewis, Daniel Hamza, Geraint Jones, Robert A. Stockman<\/p>\n

Abstract<\/strong><\/p>\n

The application of a tandem condensation\/cyclisation\/[3+2]-cycloaddition\/elimination reaction gives an sp3-rich tricyclic pyrazoline scaffold with two ethyl esters in a single step from a simple linear starting material. The successive hydrolysis and cyclisation (with Boc anhydride) of these 3-dimensional architectures, generates unprecedented 16-membered macrocyclic bisanhydrides (characterised by XRD). Selective amidations could then be achieved by ring opening with a primary amine followed by HATU-promoted amide coupling to yield an sp3-rich natural product-like library.<\/p>\n

Ref:<\/strong>\u00a0Bioorgan. Med. Chem., 23, (11), 2621 – 2628<\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":0,"template":"","category":[1],"resource_tag":[],"class_list":["post-2422","journal-paper","type-journal-paper","status-publish","hentry","category-uncategorized"],"acf":[],"yoast_head":"\nCombining two-directional synthesis and tandem reactions - Part 21: Exploitation of a dimeric macrocycle for chain terminus differentiation and synthesis of an sp3-rich library - Sygnature<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/combining-two-directional-synthesis-and-tandem-reactions-part-21-exploitation-of-a-dimeric-macrocycle-for-chain-terminus-differentiation-and-synthesis-of-an-sp3-rich-library\/\" \/>\n<meta property=\"og:locale\" content=\"fr_CA\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Combining two-directional synthesis and tandem reactions - 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