新产品编号:1342045
Chemical Name: 2-[(E)-2-(3,4-Dihydroxyphenyl)vinyl]-8-hydroxyquinoline-7-carboxylic acid
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:8-Hydroxyquinaldine (I) reacts with KOH in refluxing toluene.Treatment with CO2 and acidification with HCl then affords carboxylic acid (II).Condensation of 8-hydroxy-7-quinaldic acid (II) with 3,4-diacetoxybenzaldehyde (III) in refluxing acetic anhydride (Ac2O) followed by treatment with a refluxing mixture of pyridine/H2O affords the desired product.
📌 参考资料/链接：
参考文献标题:Quinoline derivs.,having in particular antiviral properties,preparation and biological applications thereof
文献作者:Desmaele,D.; Auclair,C.; D'Angelo,J.; Subra,F.; Mouscadet,J.-F.; Mekouar,K.(CNRS (Centre National de la Recherche Scientifique))
参考来源:WO 9845269
📄 详细内容
合成路线:8-Hydroxyquinaldine (I) reacts with KOH in refluxing toluene.Treatment with CO2 and acidification with HCl then affords carboxylic acid (II).Condensation of 8-hydroxy-7-quinaldic acid (II) with 3,4-diacetoxybenzaldehyde (III) in refluxing acetic anhydride (Ac2O) followed by treatment with a refluxing mixture of pyridine/H2O affords the desired product.
参考文献标题:Styrylquinoline derivatives: A new class of potent HIV-1 integrase inhibitors that block HIV-1 replication in CEM cells
文献作者:Mekouar,K.; Mouscadet,J.-F.; Desma雔e,D.; Subra,F.; Leh,H.; Savoure,D.; Auclair,C.; D'Angelo,J.
参考来源:J Med Chem 1998,41(15),2846
合成路线:8-Hydroxyquinaldine (I) reacts with KOH in refluxing toluene.Treatment with CO2 and acidification with HCl then affords carboxylic acid (II).Condensation of 8-hydroxy-7-quinaldic acid (II) with 3,4-diacetoxybenzaldehyde (III) in refluxing acetic anhydride (Ac2O) followed by treatment with a refluxing mixture of pyridine/H2O affords the desired product.
参考文献标题:Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture
文献作者:Zouhiri,F.; Mouscdet,J.F.; Mekouar,K.; Desma雔e,D.; Savour? D.; Leh,H.; Subra,F.; Le Bret,M.; Auclair,C.; D'Angelo,J.
参考来源:J Med Chem 2000,43(8),1533