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Synthesis, identification and molecular docking studies of N-functionalized piperidine derivatives linked to 1,2,3-triazole ring
Synthetic Communications ( IF 2.1 ) Pub Date : 2020-06-16 , DOI: 10.1080/00397911.2020.1776876 Rafid S. Dawood 1 , Sudad A. Dayl 1
Synthetic Communications ( IF 2.1 ) Pub Date : 2020-06-16 , DOI: 10.1080/00397911.2020.1776876 Rafid S. Dawood 1 , Sudad A. Dayl 1
Affiliation
Abstract New derivatives of piperidine bearing a 1,2,3-triazole ring designed and synthesized smoothly over six steps from N-protected piperidone-4-one. These steps included reduction of the carbonyl group/tosylation of the resulting alcohol providing tosyl derivative in a good yield, followed by nucleophilic substitution and Cu-catalysed azide-alkyne cycloaddition. By removing the protecting group and functionalizing amine group via reductive amination gave the desired design in moderate to very good yields. Molecular modeling studies of these compounds predicted possible binding modes into the active site of dopamine receptor D2. Graphical Abstract
中文翻译:
与1,2,3-三唑环相连的N-官能化哌啶衍生物的合成、鉴定和分子对接研究
摘要 带有 1,2,3-三唑环的哌啶新衍生物由 N-保护的哌啶酮-4-one 经过六个步骤设计和合成。这些步骤包括还原所得醇的羰基/甲苯磺酰化,以良好的产率提供甲苯磺酰衍生物,然后是亲核取代和铜催化的叠氮-炔环加成。通过去除保护基团并通过还原胺化将胺基团官能化,以中等至非常好的产率得到所需的设计。这些化合物的分子模型研究预测了多巴胺受体 D2 活性位点的可能结合模式。图形概要
更新日期:2020-06-16
中文翻译:
与1,2,3-三唑环相连的N-官能化哌啶衍生物的合成、鉴定和分子对接研究
摘要 带有 1,2,3-三唑环的哌啶新衍生物由 N-保护的哌啶酮-4-one 经过六个步骤设计和合成。这些步骤包括还原所得醇的羰基/甲苯磺酰化,以良好的产率提供甲苯磺酰衍生物,然后是亲核取代和铜催化的叠氮-炔环加成。通过去除保护基团并通过还原胺化将胺基团官能化,以中等至非常好的产率得到所需的设计。这些化合物的分子模型研究预测了多巴胺受体 D2 活性位点的可能结合模式。图形概要