ArticleThe Journal of organic chemistry2025
Time-Reduced N-Methylation: Exploring a Faster Synthesis Technique.
Article in The Journal of organic chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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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.
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1 citing paper in PubMed.
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Backbone N-methylation is a pivotal peptide modification that enhances lipophilicity, metabolic stability, and binding affinity or specificity, thereby improving bioactive peptides' bioavailability. Substitution of a backbone amide hydrogen with a methyl group is a three-step procedure which is fully integrated with solid-phase peptide synthesis strategy and usually takes about 4 h. We have revolutionized this process by optimizing the method and slashing the total N-methylation procedure time from 4 h to just 40 min. Moreover, we demonstrate that N-methylation can be equally efficient regardless of the laboratory equipment used, such as a standard laboratory shaker, microwave synthesizer, or common ultrasonic bath. Our study not only results in acceleration of the N-methylation process during solid-phase peptide synthesis but also offers a flexible choice of laboratory equipment, making peptide modifications more efficient and achievable.
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