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Pd-catalysed general access to 7-membered N/O-heterocyclic compounds as potential agents against inflammation
Chemical Communications ( IF 4.3 ) Pub Date : 2021-09-03 , DOI: 10.1039/d1cc04140a B Thirupataiah 1, 2 , Gangireddy Sujeevan Reddy 1, 2 , Guntipally Mounika 1 , Jetta Sandeep Kumar 1, 2 , Kazi Amirul Hossain 1 , Jayesh Mudgal 2 , Jessy E Mathew 2 , Gautham G Shenoy 2 , Marina Rajadurai 1 , Kishore V L Parsa 1 , Manojit Pal 1
Chemical Communications ( IF 4.3 ) Pub Date : 2021-09-03 , DOI: 10.1039/d1cc04140a B Thirupataiah 1, 2 , Gangireddy Sujeevan Reddy 1, 2 , Guntipally Mounika 1 , Jetta Sandeep Kumar 1, 2 , Kazi Amirul Hossain 1 , Jayesh Mudgal 2 , Jessy E Mathew 2 , Gautham G Shenoy 2 , Marina Rajadurai 1 , Kishore V L Parsa 1 , Manojit Pal 1
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A Pd-catalysed regioselective synthesis of 4,5-disubstituted 7-membered N/O-heterocycles was achieved via the 7-endo-dig cyclization followed by C–C bond formation of 2-(1-alkynyl)phenylacetamide. The ligand/additive free cascade reaction proceeded in the presence of PdCl2 in aqueous MeCN when the separate and individual use of methyl vinyl ketone and allyl bromide generally afforded an O- and N-heterocycle, respectively. The pharmacological assay was performed to identify the first example of a 1H-benzo[d]azepin-2(3H)-one based novel inhibitor of PDE4B.
中文翻译：
Pd 催化一般获得 7 元 N/O-杂环化合物作为抗炎症的潜在药物
钯催化的4,5-二取代的7元N / O杂环区域选择性合成达到经由7-内切挖环化，接着为C-C键形成2-（1-炔基）苯基乙酰胺的。当单独和单独使用甲基乙烯基酮和烯丙基溴通常分别提供O-和N-杂环时，配体/无添加剂的级联反应在PdCl 2的存在下在MeCN水溶液中进行。进行药理学试验以鉴定基于 1 H- benzo[ d ]azepin-2( 3H )-one 的新型 PDE4B 抑制剂的第一个实例。
更新日期：2021-09-13
中文翻译：
Pd 催化一般获得 7 元 N/O-杂环化合物作为抗炎症的潜在药物
钯催化的4,5-二取代的7元N / O杂环区域选择性合成达到经由7-内切挖环化，接着为C-C键形成2-（1-炔基）苯基乙酰胺的。当单独和单独使用甲基乙烯基酮和烯丙基溴通常分别提供O-和N-杂环时，配体/无添加剂的级联反应在PdCl 2的存在下在MeCN水溶液中进行。进行药理学试验以鉴定基于 1 H- benzo[ d ]azepin-2( 3H )-one 的新型 PDE4B 抑制剂的第一个实例。
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