{"doi":"10.1002/chem.202500751","title":"A Tetrazine‐Based Synthesis for Accessing Underutilized Aza‐Indole Analogues","abstract":"Aza-indole functionalities fill an important role in drug discovery. While indoles are considered privileged scaffolds, aza-indoles allow for better pharmacological properties and on-target activities. Synthetic approaches to access aza-indoles are limited, with pyrazolopyridazines being some of the scarcest aza-indoles. To provide access to these underutilized cores, a synthetic approach utilizing a reaction cascade between a protected propargylhydrazine and dichlorotetrazine has been developed. In addition, a variety of methods were developed to access each position on the core for late-stage functionalization. This method offers an expedited synthetic route to a rare aza-indole scaffold with superior physiochemical properties when compared to indole analogues.","journal":"Chemistry - A European Journal","year":2025,"id":551909,"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":1,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9547,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2025-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1448176,"name":"Katarina Selewski","orcid":null,"position":1,"is_corresponding":false},{"id":336049,"name":"Jetze J. Tepe","orcid":"0000-0001-5467-5589","position":2,"is_corresponding":false},{"id":1392734,"name":"Evan Savelson","orcid":"0000-0001-8963-3071","position":0,"is_corresponding":true}],"reference_count":42,"raw_metadata":null,"created_at":"2026-07-19T02:54:29.318076Z","pmid":"40035507","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":[]}