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Record W4386254646 · doi:10.1002/ejoc.202300419

Activation and Deactivation of Benzylic C−H Bonds Guided by Stereoelectronic Effects in Hydrogen Atom Transfer from Amides and Amines to Alkoxyl Radicals

2023· article· en· W4386254646 on OpenAlexaff
Sergio Sisti, Fabio Ioele, Filippo Scarchilli, Marco Galeotti, Gino A. DiLabio, Michela Salamone, Massimo Bietti

Bibliographic record

VenueEuropean Journal of Organic Chemistry · 2023
Typearticle
Languageen
FieldChemistry
TopicRadical Photochemical Reactions
Canadian institutionsUniversity of British Columbia, Okanagan CampusUniversity of British Columbia
Fundersnot available
KeywordsChemistrySteric effectsAmideRadicalLone pairIsoindolineAlkoxy groupMedicinal chemistryStereochemistryHydrogen bondAmine gas treatingAlkylPhotochemistryMoleculeOrganic chemistry

Abstract

fetched live from OpenAlex

Abstract Kinetic and product studies on the reactions of tert ‐alkoxyl radicals with secondary and tertiary alkanamides bearing benzylic α‐C−H bonds, isoindoline, tetrahydroisoquinoline and the corresponding N ‐acetyl derivatives were carried out. Product studies on the reactions with the tert ‐butoxyl radical ( t BuO⋅) point toward exclusive HAT from the benzylic α‐C−H bonds. Comparison of the k H values measured for reaction with the cumyloxyl radical (CumO⋅) with those obtained previously for the corresponding reactions of N ‐alkyl‐ and N,N ‐dialkylalkanamides, are indicative of a lack of benzylic activation and the operation of steric and stereoelectronic effects. Compared to N ‐methyl and N ‐ethyl groups, the presence of N ‐benzyl groups increases the barrier required to reach the optimal conformation for HAT, where the α‐C−H bond to be cleaved is perpendicular to the plane of the amide, precluding concurrent overlap with the phenyl π‐system. When the benzylic α‐C−H bonds are in a conformation that allows for optimal overlap with both the phenyl π‐system and the amide π‐system or amine nitrogen lone pair, as in the isoindoline and tetrahydroisoquinoline derivatives, increases in k H that exceed 2‐orders of magnitude were observed, highlighting the strong contribution provided by stereoelectronic activation to these HAT processes.

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.

How this classification was reachedexpand

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 categoriesnone
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 score0.003
Threshold uncertainty score0.781

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.001
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

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 head0.008
GPT teacher head0.223
Teacher spread0.215 · 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

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations5
Published2023
Admission routes1
Has abstractyes

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