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Record W4401655604 · doi:10.1002/adsc.202400862

Shaking Up the Friedländer Reaction: Rapid, Scalable Mechanochemical Synthesis of Polyaryl‐Substituted Quinolines

2024· article· en· W4401655604 on OpenAlex

Why this work is in the frame

A frame that forgets how it found something cannot be audited. These are the routes that admitted this work.

affAt least one author lists a Canadian institution in the pinned OpenAlex snapshot.
fundA Canadian funder is recorded on the work.

Bibliographic record

VenueAdvanced Synthesis & Catalysis · 2024
Typearticle
Languageen
FieldChemistry
TopicSynthesis and Reactivity of Heterocycles
Canadian institutionsConcordia UniversityMcGill UniversityCentre in Green Chemistry and Catalysis
FundersFonds Québécois de la Recherche sur la Nature et les TechnologiesMcGill University
KeywordsChemistryChemical engineering

Abstract

fetched live from OpenAlex

Abstract Quinolines are ubiquitous heterocyclic aromatic scaffolds, which can be found in many natural and synthetic products. They are highly valued for their pharmacological and electrochemical properties, encouraging the discovery of new routes for quinoline synthesis and diversification. In particular, polyaryl‐substituted quinolines have recently surged as useful substrates for a wide variety of applications, yet their synthetic routes remain difficult and inefficient. Herein, we report a rapid and novel mechanochemical Friedländer synthesis of polyaryl‐substituted quinolines under basic conditions using ball milling. The optimized reaction conditions resulted in moderate to excellent yields ranging from 48% to >95% and demonstrated broad functional group tolerance at 1 hour reaction times. We further show a new route for the synthesis of photocatalyst DPQN 2,4−di−OMe and photo‐ligand PPQN 2,4−di−OMe as well as OLED donor‐acceptor pCzPPQ, electron transport material oligoquinoline TQB and organic semiconductor DPA. A gram scale reaction was also achieved using Resonant Acoustic Mixing (RAM), providing an isolated yield of 87% after a simple recrystallization in ethanol.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.001
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow), Insufficient payload (model declined to judge)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.223
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.001
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0010.001
Bibliometrics0.0000.001
Science and technology studies0.0000.000
Scholarly communication0.0000.001
Open science0.0010.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0010.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.014
GPT teacher head0.250
Teacher spread0.236 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it