Protocol for the synthesis of N-Alkyl bromomaleimide linkers

Herein a straightforward and efficient method for synthesizing bromomaleimides with varied carbon chain lengths to modulate molecular properties has been reported. Compounds <b>1-4</b> incorporate a single bromomaleimide unit, while compound <b>5</b> features two, enabling dual functionalization. This synthetic approach consistently yields high-purity products in good to excellent yields, with compound <b>5</b> offering potential for dual payload conjugation due to its bifunctional structure. The key highlights are: 1. Bromomaleimides offers exceptional stability compared to maleimides counterparts 2. Highly selective for Cysteine modification.

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Journal
MethodsX
Published
2026-01-29
DOI
https://doi.org/10.1016/j.mex.2026.103809
Primary Topic
Catalytic Cross-Coupling Reactions
Type
article
Field-Weighted Citation Impact
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article

Protocol for the synthesis of N-Alkyl bromomaleimide linkers

Beatriz G. de la Torre, Aparna Sharma, Jessica T. Mlongo, Fernando Albericio
MethodsX
Catalytic Cross-Coupling Reactions
article

Protocol for the synthesis of N-Alkyl bromomaleimide linkers

Beatriz G. de la Torre, Aparna Sharma, Jessica T. Mlongo, Fernando Albericio
article en

Abstract

Herein a straightforward and efficient method for synthesizing bromomaleimides with varied carbon chain lengths to modulate molecular properties has been reported. Compounds <b>1-4</b> incorporate a single bromomaleimide unit, while compound <b>5</b> features two, enabling dual functionalization. This synthetic approach consistently yields high-purity products in good to excellent yields, with compound <b>5</b> offering potential for dual payload conjugation due to its bifunctional structure. The key highlights are: 1. Bromomaleimides offers exceptional stability compared to maleimides counterparts 2. Highly selective for Cysteine modification.

MethodsXVol. 16
Universitat de Barcelona (ES), University of KwaZulu-Natal (ZA)
Openalex Percentile: Top 73%
Catalytic Cross-Coupling Reactions
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