{"doi":"10.1021/jacs.4c05940","title":"A General Three-Component Alkyl Petasis Boron–Mannich Reaction","abstract":"Aryl amines are one of the most common moieties in biologically active molecules, and approximately 37% of drug candidates contain aromatic amines. Recent advancements in medicinal chemistry, coined “escaping from flatland”, have led to a greater focus on accessing highly functionalized C ( sp 3 )-rich amines to improve the physicochemical and pharmacokinetic properties of compounds. This article presents a modular and operationally straightforward three-component alkyl Petasis boron–Mannich (APBM) reaction that utilizes ubiquitous starting materials, including amines, aldehydes, and alkyl boronates. By adaptation of this transformation to high-throughput experimentation (HTE), it offers rapid access to an array of diverse C( sp 3 )-rich complex amines, amenable for rapid identification of drug candidates.","journal":"Journal of the American Chemical Society","year":2024,"id":421166,"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":31,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9573,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2024-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":725762,"name":"Jet Tsien","orcid":"0000-0002-2052-8051","position":1,"is_corresponding":false},{"id":246768,"name":"Si-Jie Chen","orcid":"0000-0001-9836-6892","position":2,"is_corresponding":false},{"id":1012855,"name":"May Kong","orcid":null,"position":3,"is_corresponding":false},{"id":1027184,"name":"Rohan R. Merchant","orcid":"0000-0002-5472-8780","position":4,"is_corresponding":false},{"id":569064,"name":"Yuzuru Kanda","orcid":"0000-0003-2200-2667","position":5,"is_corresponding":false},{"id":257961,"name":"Tian Qin","orcid":"0000-0001-7225-3224","position":6,"is_corresponding":false},{"id":1199182,"name":"Chao Hu","orcid":"0000-0003-3237-5934","position":0,"is_corresponding":true}],"reference_count":56,"raw_metadata":null,"created_at":"2026-07-19T01:57:36.298171Z","pmid":"39072677","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":[]}