Evidence map›Paper›PMID 40470328›Full record

ArticleInnovation (Cambridge (Mass.))2025

Oxidant-free cross-dehydrogenative oxyalkylation enables late-stage functionalization of drugs.

Weiqiu Liang, Jiahao Li, Jianbin Li, Chengda Wu, Zhiyu Tu, Bo-Shuai Mu, Yang Xu, Longlong Song, Mengxin Xu, Xi-Yang Cui and 2 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Innovation (Cambridge (Mass.)), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

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 registry

The 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 literature

Who cites it

1 citing paper in PubMed.

  1. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors.

Weiqiu LiangBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Jiahao LiBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Jianbin LiSchool of Science and Engineering, The Chinese University of Hong Kong, Shenzhen 518172, China.
Chengda WuBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Zhiyu TuBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Bo-Shuai MuBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Yang XuBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Longlong SongBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Mengxin XuChangping Laboratory, Beijing 102206, China.
Xi-Yang CuiBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Chao-Jun LiDepartment of Chemistry, McGill University, Montréal, QC H3A 0B8, Canada.
Zhibo LiuBeijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Late-stage functionalization is an attractive strategy that allows chemists to bypass lengthy synthetic processes, facilitating the rapid generation of drug analogs with potentially enhanced pharmacokinetic and pharmacological properties. This study describes a novel approach for cross-dehydrogenative oxyalkylation, leveraging a unique γ-ray-enabled photoredox process to generate oxyalkyl radicals, followed by a Minisci-type addition in an aqueous solution. The metal- and oxidant-free aqueous conditions, coupled with excellent functional group compatibility, establish this method as a versatile protocol for the late-stage oxyalkylation of unprotected, structurally complex drug molecules. Notably, this method demonstrated improved pharmacokinetics in hydroxymethylated fibroblast activation protein inhibitor (FAPI) molecules, highlighting its potential to accelerate drug discovery efforts.

Indexed as

ionizing radiationlate-stage functionalizationminisci reaction

Identifiers

PMID40470328
PMCPMC12131014

What OpenQuestion holds

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LicenceCC BY-NC-ND
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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.