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Here we present a robust and scalable, redox-neutral C\u2013H amination strategy that overcomes these challenges through the synergistic use of readily installed and traceless imidates with internal oxidizing N\u2013OPiv reagents. This redox-neutral C\u2013H amination features unprecedented tolerance across 12 classes of strongly coordinating heterocycles, including the notoriously challenging pyridines and azole. The resulting imidate products serve as versatile linchpins for direct transformation into nitriles, carboxylic acids, tetrazoles, and amines, enabling rapid molecular diversification. This methodology facilitates regiospecific late-stage modification of pharmaceuticals, such as celecoxib and letrozole analogues, and expedites the construction of a celecoxib-focused molecular library, from which novel antibacterial derivatives active against Staphylococcus aureus were identified.<\/jats:p>","DOI":"10.1021\/acs.orglett.6c02565","type":"journal-article","created":{"date-parts":[[2026,8,19]],"date-time":"2026-08-19T03:02:34Z","timestamp":1787108554000},"page":"10691-10696","source":"Crossref","is-referenced-by-count":1,"title":["Transformable\nImidates Enabled Regiodivergent and\nRedox-Neutral C\u2013H Amination That Tolerated Strongly Coordinating\nHeterocycles"],"prefix":"10.1021","volume":"28","author":[{"given":"Xiaojian","family":"Chen","sequence":"first","affiliation":[{"name":"Guangdong University of Technology , , ,","place":["Guangzhou, China, 510006"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jun","family":"Zhang","sequence":"additional","affiliation":[{"name":"Guangdong University of Technology , , ,","place":["Guangzhou, China, 510006"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9513-6899","authenticated-orcid":true,"given":"Yang","family":"Gao","sequence":"additional","affiliation":[{"name":"Guangdong University of Technology , , ,","place":["Guangzhou, China, 510006"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0818-6028","authenticated-orcid":true,"given":"Qian","family":"Chen","sequence":"additional","affiliation":[{"name":"Guangdong University of Technology , , ,","place":["Guangzhou, China, 510006"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4124-6026","authenticated-orcid":true,"given":"Yanping","family":"Huo","sequence":"additional","affiliation":[{"name":"Guangdong University of Technology , , ,","place":["Guangzhou, China, 510006"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4014-6712","authenticated-orcid":true,"given":"Xianwei","family":"Li","sequence":"additional","affiliation":[{"name":"Guangdong University of Technology , , ,","place":["Guangzhou, China, 510006"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2026,8,18]]},"reference":[{"key":"2026090200175287900_cit1a","doi-asserted-by":"publisher","first-page":"27","DOI":"10.1039\/C0SC00331J","article-title":"Dialkylbiaryl Phosphines in Pd-catalyzed\nAmination: a User\u2019s guide","volume":"2","author":"Surry","year":"2011","journal-title":"Chem. 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