Ramesha Thongolla , Ummareddy Venkata Subba Reddy , Sailam Sri Gogula , Empati Raja Sekhar , Puchakayala Muralidhar Reddy , Anren Hu
{"title":"以苦味酸为催化剂的N-Boc保护胺的无溶剂环保绿色方案","authors":"Ramesha Thongolla , Ummareddy Venkata Subba Reddy , Sailam Sri Gogula , Empati Raja Sekhar , Puchakayala Muralidhar Reddy , Anren Hu","doi":"10.1016/j.tgchem.2024.100061","DOIUrl":null,"url":null,"abstract":"<div><div>We have developed an environmentally conscious green protocol to protect amine functional groups in drug discovery and the total synthesis of biologically active natural products. This method utilizes di-<em>tert</em>-butyl dicarbonate ((Boc)<sub>2</sub>O) to protect aromatic and aliphatic amines, with readily available picric acid (2 mol%) serving as a Brønsted acid catalyst. This approach enables rapid and high-yield (up to 98 %) protection of amines under completely solvent-free and eco-friendly conditions, thereby promoting a cleaner and more sustainable synthetic process.</div></div>","PeriodicalId":101215,"journal":{"name":"Tetrahedron Green Chem","volume":"5 ","pages":"Article 100061"},"PeriodicalIF":0.0000,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Solvent-free and eco-friendly green protocol for N-Boc Protection of amines using picric acid as a catalyst\",\"authors\":\"Ramesha Thongolla , Ummareddy Venkata Subba Reddy , Sailam Sri Gogula , Empati Raja Sekhar , Puchakayala Muralidhar Reddy , Anren Hu\",\"doi\":\"10.1016/j.tgchem.2024.100061\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>We have developed an environmentally conscious green protocol to protect amine functional groups in drug discovery and the total synthesis of biologically active natural products. This method utilizes di-<em>tert</em>-butyl dicarbonate ((Boc)<sub>2</sub>O) to protect aromatic and aliphatic amines, with readily available picric acid (2 mol%) serving as a Brønsted acid catalyst. This approach enables rapid and high-yield (up to 98 %) protection of amines under completely solvent-free and eco-friendly conditions, thereby promoting a cleaner and more sustainable synthetic process.</div></div>\",\"PeriodicalId\":101215,\"journal\":{\"name\":\"Tetrahedron Green Chem\",\"volume\":\"5 \",\"pages\":\"Article 100061\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2025-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Tetrahedron Green Chem\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2773223124000268\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/12/13 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Tetrahedron Green Chem","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2773223124000268","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/12/13 0:00:00","PubModel":"Epub","JCR":"","JCRName":"","Score":null,"Total":0}
Solvent-free and eco-friendly green protocol for N-Boc Protection of amines using picric acid as a catalyst
We have developed an environmentally conscious green protocol to protect amine functional groups in drug discovery and the total synthesis of biologically active natural products. This method utilizes di-tert-butyl dicarbonate ((Boc)2O) to protect aromatic and aliphatic amines, with readily available picric acid (2 mol%) serving as a Brønsted acid catalyst. This approach enables rapid and high-yield (up to 98 %) protection of amines under completely solvent-free and eco-friendly conditions, thereby promoting a cleaner and more sustainable synthetic process.
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