{"doi":"10.1002/jlcr.4065","title":"A practical protocol for large‐scale copper‐mediated radioiodination of organoboronic precursors: Radiosynthesis of [<sup>123</sup>I]KX‐1 for Auger radiotherapy","abstract":"Nucleophilic copper‐mediated radioiodination (CMRI) of organoboronic precursors with radioiodides is a promising method of radioiodination. The previously reported CMRI has demonstrated its great potential and scope of labeling for the radiosynthesis of radioiodine‐labeled compounds. However, the reported protocols (using a small amount/volume of radioactivity) are practically not reproducible in large‐scale CMRI, in which the radioactivity was usually provided in a bulk alkaline solution. A large amount of water and a strong base are incompatible with CMRI. To overcome these issues in large‐scale CMRI, we have developed a simple protocol for large‐scale CMRI. The bulk water was removed under a flow of inert gas at 110°C, and the strong base (i.e., NaOH) was neutralized with an acid, pyridinium p ‐toluenesulfonate or p ‐toluenesulfonic acid. In the model reactions of [ 123 I]KX‐1, a PARP‐1 radioligand for Auger radiotherapy, radiochemical conversions were significantly improved after neutralization of the base, and the addition of additional acids was tolerated and favorable for the reactions. Using this protocol, [ 123 I]KX‐1 was radiosynthesized from 20 mCi (0.74 GBq) of [ 123 I]iodide in high radiochemical yields, high radiochemical purity, and high molar activity. This protocol should be applicable to the radiosynthesis of other compounds with radioiodine via CMRI.","journal":"Journal of Labelled Compounds and Radiopharmaceuticals","year":2023,"id":383733,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":2,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.95,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2023-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":391865,"name":"Wenhua Chu","orcid":null,"position":1,"is_corresponding":false},{"id":364748,"name":"Jinbin Xu","orcid":"0000-0002-2120-8287","position":2,"is_corresponding":false},{"id":391204,"name":"Dong Zhou","orcid":"0000-0002-6707-4878","position":0,"is_corresponding":true}],"reference_count":13,"raw_metadata":null,"created_at":"2026-07-19T01:17:29.050285Z","pmid":"37735764","pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}