{"id":6647,"date":"2023-02-17T07:15:18","date_gmt":"2023-02-17T07:15:18","guid":{"rendered":"https:\/\/beta.nanion.de\/resource_library\/2022-palladium-catalyzed-%ce%b1-arylation-of-cyclic-%ce%b2-dicarbonyl-compounds-for-the-synthesis-of-cav1-3-inhibitors\/"},"modified":"2023-02-17T07:15:19","modified_gmt":"2023-02-17T07:15:19","slug":"2022-palladium-catalyzed-%ce%b1-arylation-of-cyclic-%ce%b2-dicarbonyl-compounds-for-the-synthesis-of-cav1-3-inhibitors","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2022-palladium-catalyzed-%ce%b1-arylation-of-cyclic-%ce%b2-dicarbonyl-compounds-for-the-synthesis-of-cav1-3-inhibitors\/","title":{"rendered":"2022 &#8211; Palladium-Catalyzed \u03b1-Arylation of Cyclic \u03b2-Dicarbonyl Compounds for the Synthesis of CaV1.3 Inhibitors"},"content":{"rendered":"<p>Cyclic \u03b1-aryl \u03b2-dicarbonyl derivatives are important scaffolds in medicinal chemistry. Palladium-catalyzed coupling reactions of haloarenes were conducted with diverse five- to seven-membered cyclic \u03b2-dicarbonyl derivatives including barbiturate, pyrazolidine-3,5-dione, and 1,4-diazepane-5,7-dione. The coupling reactions of various para- or meta-substituted aryl halides occurred efficiently when Pd(t-Bu3P)2, Xphos, and Cs2CO3\u00a0were used under 1,4-dioxane reflux conditions. Although the couplings of ortho-substituted aryl halides with pyrazolidine-3,5-dione and 1,4-diazepane-5,7-dione were moderate, the coupling with barbiturate was limited. Using the optimized reaction conditions, we synthesized several 5-aryl barbiturates as new scaffolds of CaV1.3 Ca<sup>2+<\/sup>\u00a0channel inhibitors. Among the synthesized molecules,\u00a014e\u00a0was the most potent CaV1.3 inhibitor with an IC<sub>50<\/sub>\u00a0of 1.42 \u03bcM.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[42],"resource_type":[75],"application_areas":[50,76],"therapeutic_areas":[55],"target_categories":[61],"target_families":[340],"targets":[282],"resource_keyword":[],"class_list":["post-6647","resource_library","type-resource_library","status-publish","hentry","products_tags-syncropatch-384","resource_type-publication","application_areas-ion-channels","application_areas-drug-discovery","therapeutic_areas-cns","target_categories-voltage-gated-ion-channels","target_families-cav-channels","targets-cav1-3"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library\/6647","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library"}],"about":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/types\/resource_library"}],"wp:attachment":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/media?parent=6647"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=6647"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=6647"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=6647"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=6647"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=6647"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=6647"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=6647"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=6647"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}