{"id":981,"date":"2018-06-21T12:22:39","date_gmt":"2018-06-21T11:22:39","guid":{"rendered":"http:\/\/www.mub.eps.manchester.ac.uk\/in-abstract\/?p=981"},"modified":"2018-09-03T11:42:35","modified_gmt":"2018-09-03T10:42:35","slug":"arylation-of-pharmaceuticals","status":"publish","type":"post","link":"https:\/\/www.mub.eps.manchester.ac.uk\/in-abstract\/arylation-of-pharmaceuticals\/","title":{"rendered":"Cyclometallated ruthenium catalyst enables late-stage directed arylation of pharmaceuticals"},"content":{"rendered":"<p><strong>New class of ruthenium catalysts allows late-stage arylation of drugs<\/strong><\/p>\n<p>Most drugs and other biologically active compounds incorporate a large number of polar functional groups, which are responsible for the observed activity. However, the presence of these polar groups increase difficulty for chemists to modify these compounds as often transition metal catalyst will be incompatible with those functionalities.<\/p>\n<p>Chemists at the University of Manchester have uncovered new mechanistic insights on the workings of ruthenium-catalysed C\u2012H arylations. This discovery has led to the design of a new class of ruthenium catalysts that present extremely high reactivity, when compared to current state-of-the-art catalysts, on C\u2012H arylation. These catalysts maintain their high reactivity under very mild conditions (e.g. room temperature), while displaying exquisite selectivity and efficiency, making them particularly suitable for the modification of highly functionalized delicate molecules such as drugs compounds. These ruthenium catalysts provide chemists with a tool to install aromatic groups at desired positions of complex molecules, opening the door to the exploration of new chemical space that would otherwise be impractical to access.<\/p>\n<div class=\"abstract-box\"><\/p>\n<ul>\n<li>Drug molecules generally contain several polar groups, often nitrogen- and oxygen-based. These can potentially coordinate catalysts and lead to catalyst poisoning or suffer reactions that decompose the molecules.<\/li>\n<li>C\u2012H arylation is a type of reaction that allows selecting one of the multiple C\u2012H bonds found in an organic molecule and replacing it with an aromatic ring through a C\u2012C bond formation.<\/li>\n<li>Late stage arylation is a specific type of C\u2012H arylation that is applicable to complex molecules, rather than just to simple ones.<\/li>\n<li>The picture shows the transformation of drugs into arylated versions upon reaction with the ruthenium &#8220;gate&#8221; catalysts.<\/li>\n<\/ul>\n<p><\/div>\n<p class=\"button\"><a target=\"blank\" href=\"https:\/\/www.nature.com\/articles\/s41557-018-0062-3\" class=\"uom-button\">To read the full article, click here - https:\/\/www.nature.com\/articles\/s41557-018-0062-3<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>New class of ruthenium catalysts allows late-stage arylation of drugs Most drugs and other biologically active compounds incorporate a large number of polar functional groups, which are responsible for the observed activity. However, the presence of these polar groups increase difficulty for chemists to modify these compounds as often transition metal catalyst will be incompatible [&hellip;]<\/p>\n","protected":false},"author":157,"featured_media":1020,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_genesis_hide_title":false,"_genesis_hide_breadcrumbs":false,"_genesis_hide_singular_image":false,"_genesis_hide_footer_widgets":false,"_genesis_custom_body_class":"","_genesis_custom_post_class":"","_genesis_layout":"","_jetpack_memberships_contains_paid_content":false,"footnotes":""},"categories":[13,3,19],"tags":[],"class_list":{"0":"post-981","1":"post","2":"type-post","3":"status-publish","4":"format-standard","5":"has-post-thumbnail","7":"category-archive","8":"category-chemistry","9":"category-edition-06","10":"entry"},"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.4 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Cyclometallated ruthenium catalyst enables late-stage directed arylation of pharmaceuticals - In Abstract<\/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.mub.eps.manchester.ac.uk\/in-abstract\/arylation-of-pharmaceuticals\/\" \/>\n<meta property=\"og:locale\" content=\"en_GB\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Cyclometallated ruthenium catalyst enables late-stage directed arylation of pharmaceuticals - In Abstract\" \/>\n<meta property=\"og:description\" content=\"New class of ruthenium catalysts allows late-stage arylation of drugs Most drugs and other biologically active compounds incorporate a large number of polar functional groups, which are responsible for the observed activity. However, the presence of these polar groups increase difficulty for chemists to modify these compounds as often transition metal catalyst will be incompatible [&hellip;]\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.mub.eps.manchester.ac.uk\/in-abstract\/arylation-of-pharmaceuticals\/\" \/>\n<meta property=\"og:site_name\" content=\"In Abstract\" \/>\n<meta property=\"article:published_time\" content=\"2018-06-21T11:22:39+00:00\" \/>\n<meta property=\"article:modified_time\" content=\"2018-09-03T10:42:35+00:00\" \/>\n<meta property=\"og:image\" content=\"https:\/\/www.mub.eps.manchester.ac.uk\/in-abstract\/wp-content\/uploads\/sites\/61\/2018\/08\/Cyclometallated-ruthenium-catalyst-enables-late-stage-directed-arylation-of-pharmaceuticals.jpg\" \/>\n\t<meta property=\"og:image:width\" content=\"890\" \/>\n\t<meta property=\"og:image:height\" content=\"350\" \/>\n\t<meta property=\"og:image:type\" content=\"image\/jpeg\" \/>\n<meta name=\"author\" content=\"Enna Bartlett\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Enna Bartlett\" \/>\n\t<meta name=\"twitter:label2\" content=\"Estimated reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\\\/\\\/schema.org\",\"@graph\":[{\"@type\":\"Article\",\"@id\":\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/arylation-of-pharmaceuticals\\\/#article\",\"isPartOf\":{\"@id\":\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/arylation-of-pharmaceuticals\\\/\"},\"author\":{\"name\":\"Enna Bartlett\",\"@id\":\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/#\\\/schema\\\/person\\\/e1ec31af6571092b97ca2fdd756e6582\"},\"headline\":\"Cyclometallated ruthenium catalyst enables late-stage directed arylation of pharmaceuticals\",\"datePublished\":\"2018-06-21T11:22:39+00:00\",\"dateModified\":\"2018-09-03T10:42:35+00:00\",\"mainEntityOfPage\":{\"@id\":\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/arylation-of-pharmaceuticals\\\/\"},\"wordCount\":321,\"commentCount\":0,\"image\":{\"@id\":\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/arylation-of-pharmaceuticals\\\/#primaryimage\"},\"thumbnailUrl\":\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/wp-content\\\/uploads\\\/sites\\\/61\\\/2018\\\/08\\\/Cyclometallated-ruthenium-catalyst-enables-late-stage-directed-arylation-of-pharmaceuticals.jpg\",\"articleSection\":[\"Archive\",\"Chemistry\",\"Edition 06\"],\"inLanguage\":\"en-GB\",\"potentialAction\":[{\"@type\":\"CommentAction\",\"name\":\"Comment\",\"target\":[\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/arylation-of-pharmaceuticals\\\/#respond\"]}]},{\"@type\":\"WebPage\",\"@id\":\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/arylation-of-pharmaceuticals\\\/\",\"url\":\"https:\\\/\\\/www.mub.eps.manchester.ac.uk\\\/in-abstract\\\/arylation-of-pharmaceuticals\\\/\",\"name\":\"Cyclometallated ruthenium catalyst enables late-stage directed arylation of pharmaceuticals - 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