{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Zong Y"],"funding":["Science, Technology and Innovation Commission of Shenzhen Municipality","Basic and Applied Basic Research Foundation of Guangdong Province","National Natural Science Foundation of China","National Key Research and Development Program of China"],"pagination":["20376-20381"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC12489802"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["16(43)"],"pubmed_abstract":["A catalytic protocol for the iridium-catalyzed dynamic kinetic resolution asymmetric hydrogenation (DKR-AH) of α-substituted tetralones to rapidly assemble various enantioenriched tetrahydronaphthols is disclosed. A wide range of enantioenriched tetrahydronaphthols were obtained in high yields and excellent stereoselectivities (up to 99% yield, up to >99.5 : 0.5 er and >20 : 1 dr). And this unique platform exhibited high efficiency for the enantioselective synthesis of (+)-elacestrant, which was approved by the FDA in 2023 for the treatment of metastatic breast cancer. Additionally, palladium-catalyzed amination of aryl chloride assisted in furnishing the gram-scale synthesis of this oral anti-tumor drug within 7 steps in 43% yield."],"journal":["Chemical science"],"pubmed_title":["Gram-scale synthesis of (+)-elacestrant streamlined by iridium-catalyzed dynamic kinetic asymmetric hydrogenation of α-substituted tetralones."],"pmcid":["PMC12489802"],"funding_grant_id":["22171129","JCYJ20240813095106009","2022B1515020055","2021YFA1500200","22302090","2022A1515110093","21991113"],"pubmed_authors":["Zou X","Zong Y","Chen GQ","Zhang X","Zhang S"],"additional_accession":[]},"is_claimable":false,"name":"Gram-scale synthesis of (+)-elacestrant streamlined by iridium-catalyzed dynamic kinetic asymmetric hydrogenation of α-substituted tetralones.","description":"A catalytic protocol for the iridium-catalyzed dynamic kinetic resolution asymmetric hydrogenation (DKR-AH) of α-substituted tetralones to rapidly assemble various enantioenriched tetrahydronaphthols is disclosed. A wide range of enantioenriched tetrahydronaphthols were obtained in high yields and excellent stereoselectivities (up to 99% yield, up to >99.5 : 0.5 er and >20 : 1 dr). And this unique platform exhibited high efficiency for the enantioselective synthesis of (+)-elacestrant, which was approved by the FDA in 2023 for the treatment of metastatic breast cancer. Additionally, palladium-catalyzed amination of aryl chloride assisted in furnishing the gram-scale synthesis of this oral anti-tumor drug within 7 steps in 43% yield.","dates":{"release":"2025-01-01T00:00:00Z","publication":"2025 Nov","modification":"2026-06-05T11:39:22.936Z","creation":"2026-05-16T03:12:57.291Z"},"accession":"S-EPMC12489802","cross_references":{"pubmed":["41050573"],"doi":["10.1039/d5sc05497d"]}}