{"title":"微波增强杂环化:使用 2-乙氧基乙醇溶剂制备 1,5-苯并硫氮杂卓的简便方法及其抗菌潜力","authors":"Gajanan Kottapalle, Dayanand Jadhav, Pravin Poul, Avinash Shinde","doi":"10.1002/jhet.4823","DOIUrl":null,"url":null,"abstract":"<p>The present research study involves synthesis of 1,5-benzothiazepines has been prepared, derived from chalcones and 2-aminothiophenol in a catalytic amount of piperidine using different solvent conditions under microwave irradiation procedure with the aim to test their antibacterial activity and effect of different solvents in the synthesis. It resulted in good yield of 1,5-benzothiazepines <b>(3a-j)</b> and proved to be an efficient and environmentally benign procedure. The synthesized compounds were characterized by conventional spectral data and screened for their in vitro antibacterial activity against four pathogenic bacteria using agar diffusion method. The traditional classical heating method takes more reaction time. So, in this study, we have tested microwave irradiation process and found that 2-ethoxy ethanol as an alternative solvent in reducing the reaction time (up to 4–6 min.) with high yield as compared with classical method. The synthesized compounds <b>3a</b>, <b>3c</b>, <b>3d</b>, <b>3e</b>, <b>3 h</b>, <b>3i</b>, <b>3j</b> exhibit good to moderate antibacterial activity.</p>","PeriodicalId":194,"journal":{"name":"Journal of Heterocyclic Chemistry","volume":"61 8","pages":"1261-1268"},"PeriodicalIF":2.0000,"publicationDate":"2024-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Microwave-enhanced heterocyclization: A convenient procedure for 1,5-benzothiazepine using 2-ethoxy ethanol solvent and its antibacterial potential\",\"authors\":\"Gajanan Kottapalle, Dayanand Jadhav, Pravin Poul, Avinash Shinde\",\"doi\":\"10.1002/jhet.4823\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>The present research study involves synthesis of 1,5-benzothiazepines has been prepared, derived from chalcones and 2-aminothiophenol in a catalytic amount of piperidine using different solvent conditions under microwave irradiation procedure with the aim to test their antibacterial activity and effect of different solvents in the synthesis. It resulted in good yield of 1,5-benzothiazepines <b>(3a-j)</b> and proved to be an efficient and environmentally benign procedure. The synthesized compounds were characterized by conventional spectral data and screened for their in vitro antibacterial activity against four pathogenic bacteria using agar diffusion method. The traditional classical heating method takes more reaction time. So, in this study, we have tested microwave irradiation process and found that 2-ethoxy ethanol as an alternative solvent in reducing the reaction time (up to 4–6 min.) with high yield as compared with classical method. The synthesized compounds <b>3a</b>, <b>3c</b>, <b>3d</b>, <b>3e</b>, <b>3 h</b>, <b>3i</b>, <b>3j</b> exhibit good to moderate antibacterial activity.</p>\",\"PeriodicalId\":194,\"journal\":{\"name\":\"Journal of Heterocyclic Chemistry\",\"volume\":\"61 8\",\"pages\":\"1261-1268\"},\"PeriodicalIF\":2.0000,\"publicationDate\":\"2024-05-31\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Heterocyclic Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1002/jhet.4823\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Heterocyclic Chemistry","FirstCategoryId":"92","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/jhet.4823","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
Microwave-enhanced heterocyclization: A convenient procedure for 1,5-benzothiazepine using 2-ethoxy ethanol solvent and its antibacterial potential
The present research study involves synthesis of 1,5-benzothiazepines has been prepared, derived from chalcones and 2-aminothiophenol in a catalytic amount of piperidine using different solvent conditions under microwave irradiation procedure with the aim to test their antibacterial activity and effect of different solvents in the synthesis. It resulted in good yield of 1,5-benzothiazepines (3a-j) and proved to be an efficient and environmentally benign procedure. The synthesized compounds were characterized by conventional spectral data and screened for their in vitro antibacterial activity against four pathogenic bacteria using agar diffusion method. The traditional classical heating method takes more reaction time. So, in this study, we have tested microwave irradiation process and found that 2-ethoxy ethanol as an alternative solvent in reducing the reaction time (up to 4–6 min.) with high yield as compared with classical method. The synthesized compounds 3a, 3c, 3d, 3e, 3 h, 3i, 3j exhibit good to moderate antibacterial activity.
期刊介绍:
The Journal of Heterocyclic Chemistry is interested in publishing research on all aspects of heterocyclic chemistry, especially development and application of efficient synthetic methodologies and strategies for the synthesis of various heterocyclic compounds. In addition, Journal of Heterocyclic Chemistry promotes research in other areas that contribute to heterocyclic synthesis/application, such as synthesis design, reaction techniques, flow chemistry and continuous processing, multiphase catalysis, green chemistry, catalyst immobilization and recycling.