{"doi":"10.1021/acs.oprd.1c00099","title":"New Scalable Synthetic Routes to <b>ELQ-300</b>, <b>ELQ-316</b>, and Other Antiparasitic Quinolones","abstract":"The endochin-like quinolone (ELQ) compound class may yield effective, safe treatments for a range of important human and animal afflictions. However, to access the public health potential of this compound series, a synthetic route needed to be devised, which would lower costs and be amenable to large-scale production. In the new synthetic route described here, a substituted β-keto ester, formed by an Ullmann reaction and subsequent acylation, is reacted with an aniline via a Conrad–Limpach reaction to produce 3-substituted 4(1H)-quinolones such as ELQ-300 and ELQ-316. This synthetic route, the first described to be truly amenable to industrial-scale production, is relatively short (five reaction steps), does not require palladium, chromatographic separation, or protecting group chemistry, and may be performed without high vacuum distillation.","journal":"Organic Process Research & Development","year":2021,"id":176588,"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":21,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.951,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2021-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":381170,"name":"Rozalia A. Dodean","orcid":"0000-0001-5002-4607","position":1,"is_corresponding":false},{"id":559426,"name":"Lisa Frueh","orcid":"0000-0002-2489-2467","position":2,"is_corresponding":false},{"id":719978,"name":"Katherine M. Liebman","orcid":null,"position":3,"is_corresponding":false},{"id":719979,"name":"Rory T. Gallagher","orcid":null,"position":4,"is_corresponding":false},{"id":369627,"name":"Haihong Jin","orcid":"0000-0001-5455-0890","position":5,"is_corresponding":false},{"id":719291,"name":"Robert T. Jacobs","orcid":"0000-0001-9669-2862","position":6,"is_corresponding":false},{"id":317898,"name":"Aaron Nilsen","orcid":"0000-0002-3827-8222","position":7,"is_corresponding":false},{"id":719292,"name":"David R. Stuart","orcid":"0000-0003-3519-9067","position":8,"is_corresponding":false},{"id":352978,"name":"J. Stone Doggett","orcid":"0000-0002-6098-1520","position":9,"is_corresponding":false},{"id":381169,"name":"Michael K. Riscoe","orcid":"0000-0002-1343-5279","position":10,"is_corresponding":false},{"id":382217,"name":"Rolf W. Winter","orcid":null,"position":11,"is_corresponding":false},{"id":382216,"name":"Sovitj Pou","orcid":null,"position":0,"is_corresponding":true}],"reference_count":42,"raw_metadata":null,"created_at":"2026-07-18T23:47:23.605867Z","pmid":"35110959","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":[]}