Evidence map›Paper›PMID 42438147›Full record

ArticleOrganic letters2026

Synthesis of 1,3-Disubstituted 3-Azabicyclo[3.2.0]heptane Libraries for Fragment-Based Drug Discovery.

Mathilde A C H Janssen, Jesper W A van der Vorm, Rico Rappard, Bart Bijleveld, Tom Dekker, Maikel Wijtmans, Iwan J P de Esch, Daniel Blanco-Ania, Floris P J T Rutjes

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Organic letters, 2026. 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
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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

9 authors.

Mathilde A C H JanssenInstitute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525 AJ Nijmegen, the Netherlands.
Jesper W A van der VormInstitute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525 AJ Nijmegen, the Netherlands.
Rico RappardInstitute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525 AJ Nijmegen, the Netherlands.
Bart BijleveldInstitute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525 AJ Nijmegen, the Netherlands.ORCID 0009-0003-2588-0315
Tom DekkerAmsterdam Institute of Molecular and Life Sciences, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.
Maikel WijtmansAmsterdam Institute of Molecular and Life Sciences, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.ORCID 0000-0001-8955-8016
Iwan J P de EschAmsterdam Institute of Molecular and Life Sciences, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.ORCID 0000-0002-1969-0238
Daniel Blanco-AniaInstitute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525 AJ Nijmegen, the Netherlands.
Floris P J T RutjesInstitute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525 AJ Nijmegen, the Netherlands.ORCID 0000-0003-1538-3852

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The 3-azabicyclo[3.2.0]heptane scaffold, yet underexplored in drug discovery, offers significant potential as a structural motif for medicinal chemistry. In this study, we present the synthesis of 1,3-disubstituted 3-azabicyclo[3.2.0]heptane derived building blocks via a 1,3-dipolar cycloaddition between the unique cyclobutene-1-sulfonyl fluoride (CBSF) building block and an azomethine ylide. To evaluate the chemical diversity and novelty of the fragments, we synthesized a covalent and a noncovalent fragment library inspired by an automated workflow. The synthesis and derivatization processes─including the formation of sulfonamides, carboxamides, ureas, and tertiary amines─are detailed, demonstrating the versatility and synthetic potential of 3-azabicyclo[3.2.0]heptane scaffolds in drug discovery.

Indexed as

Azabicyclo CompoundsDrug DiscoveryHeptanesSmall Molecule LibrariesAzo CompoundsCycloaddition ReactionMolecular StructureSulfonamidesThiosemicarbazonesAzabicyclo CompoundsAzo CompoundsazomethineHeptanesSmall Molecule LibrariesSulfonamidesThiosemicarbazones

Identifiers

PMID42438147
PMCPMC13411048

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

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.