{"title":"微波辅助条件下使用 Selectfluor 对 2H-Indazoles 进行区域选择性 C3-甲酰化反应","authors":"Manivel Pitchai, Mahammed Kaspady, Gopikumar Indasi, Rajesh Krishnan, Gururaju Sannakki Maheswarappa, Muthalagu Vetrichelvan, Arvind Mathur, Anuradha Gupta","doi":"10.1055/a-2266-3213","DOIUrl":null,"url":null,"abstract":"<p>An efficient microwave-assisted Selectfluor-mediated regioselective C3-formylation of 2<i>H</i>-indazoles bearing a variety of alkyl and aryl substituents using DMSO as the formylating agent has been developed. This methodology provides access to 3-formyl 2<i>H</i>-indazoles with moderate to excellent yields. These functionalized indazoles are potentially useful as templates for drug discovery. Control experimental results suggest that this formylation probably proceeds through a radical pathway.</p>","PeriodicalId":22135,"journal":{"name":"SynOpen","volume":null,"pages":null},"PeriodicalIF":2.0000,"publicationDate":"2024-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Regioselective C3-Formylation of 2H-Indazoles Using Selectfluor under Microwave-Assisted Conditions\",\"authors\":\"Manivel Pitchai, Mahammed Kaspady, Gopikumar Indasi, Rajesh Krishnan, Gururaju Sannakki Maheswarappa, Muthalagu Vetrichelvan, Arvind Mathur, Anuradha Gupta\",\"doi\":\"10.1055/a-2266-3213\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>An efficient microwave-assisted Selectfluor-mediated regioselective C3-formylation of 2<i>H</i>-indazoles bearing a variety of alkyl and aryl substituents using DMSO as the formylating agent has been developed. This methodology provides access to 3-formyl 2<i>H</i>-indazoles with moderate to excellent yields. These functionalized indazoles are potentially useful as templates for drug discovery. Control experimental results suggest that this formylation probably proceeds through a radical pathway.</p>\",\"PeriodicalId\":22135,\"journal\":{\"name\":\"SynOpen\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":2.0000,\"publicationDate\":\"2024-03-04\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"SynOpen\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1055/a-2266-3213\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"SynOpen","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1055/a-2266-3213","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
Regioselective C3-Formylation of 2H-Indazoles Using Selectfluor under Microwave-Assisted Conditions
An efficient microwave-assisted Selectfluor-mediated regioselective C3-formylation of 2H-indazoles bearing a variety of alkyl and aryl substituents using DMSO as the formylating agent has been developed. This methodology provides access to 3-formyl 2H-indazoles with moderate to excellent yields. These functionalized indazoles are potentially useful as templates for drug discovery. Control experimental results suggest that this formylation probably proceeds through a radical pathway.
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