ArticleJACS Au2025
Hexafluoroisopropanol-Mediated Cascade Cyclization for Construction of α‑Amino-γ-spirolactones.
Haoran Li, Fangting Huang, Claire Miesch, Robert J Mayer, Yuwei Liu, Jianlian Huang, Lei Ma, Zhongyi Zeng, Zhi Zhou, David Lebœuf and 2 more
Abstract read
In one paragraphArticle in JACS Au, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
2 · The registryThe trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
3 · Its place in the literatureWho cites it
0 citing papers in PubMed.
No citing paper in PubMed yet.
4 · The recordCorrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
5 · Who and what moneyAuthors and funding
12 authors.
Haoran LiKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.
Fangting HuangKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.
Claire MieschInstitut Laboratoire d'Innovation Moléculaire et Applications (LIMA) CNRS UMR 70042, Université de Strasbourg, Université de Haute-Alsace 25 rue Becquerel, 67000 Strasbourg, France.
Yuwei LiuKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.
Jianlian HuangKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.
Lei MaKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.
Zhongyi ZengKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.ORCID https://orcid.org/0000-0003-3366-7592 Zhi ZhouKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.ORCID https://orcid.org/0000-0002-6521-8946 David LebœufInstitut Laboratoire d'Innovation Moléculaire et Applications (LIMA) CNRS UMR 70042, Université de Strasbourg, Université de Haute-Alsace 25 rue Becquerel, 67000 Strasbourg, France.ORCID https://orcid.org/0000-0001-5720-7609 Wei YiKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.ORCID https://orcid.org/0000-0001-7936-9326 Shengdong WangKey Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, Guangdong 511436, China.ORCID https://orcid.org/0000-0001-7431-2515 Funding
No grant is acknowledged in the PubMed record.
6 · The paper itselfAbstract
Given the ubiquity of spirolactones in pharmaceutical agents, natural products, and small-molecule chemical probes, considerable research has been devoted to streamlining their synthesis. Yet, the preparation of α-amino-γ-spirolactones, which combine two key motifs in drug discoveryspirocycle and amine unitsremains underdeveloped. Here, we demonstrate that readily accessible building blocksamines, glyoxylic acid, and unactivated alkenescan be rapidly converted to complex three-dimensional α-amino-γ-spirolactones and related compounds employing a hexafluoroisopropanol-promoted cascade cyclization. This protocol is general, efficient, scalable, and applicable to the mid- and late-stage functionalization of medicinally relevant molecules, while displaying excellent sustainability metrics. All those features, along with preliminary results indicating the potential bioactivity of spirolactones against cancer cells, make the reported methodology a promising tool for drug discovery.
Indexed as
aza-Prins reactionbioactivityhexafluoroisopropanollate-stage functionalizationspirolactones
Identifiers
PMID41311951
PMCPMC12648336
What OpenQuestion holds
Textmetadata
LicenceCC BY-NC-ND
Read underepoch 390