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  Mengmeng Jia,Heng Zhang,Yongjia Lin,Dimei Chen,Yanmei Chen,Yuanzhi Xia Org. Biomol. Chem. 2018 16 3615
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• Solvents and Organic Chemicals Organic Compounds Benzenoids Benzene and substituted derivatives Anilides

Recent Advances in the Study of Formamide,N-(2-bromophenyl)- (CAS: 10113-38-9) and Its Applications in Chemical Biology and Pharmaceutical Research

Formamide,N-(2-bromophenyl)- (CAS: 10113-38-9) is a brominated aromatic formamide derivative that has recently gained attention in chemical biology and pharmaceutical research due to its unique structural properties and potential therapeutic applications. This compound, characterized by the presence of a bromine atom at the ortho position of the phenyl ring, serves as a versatile intermediate in organic synthesis and has shown promise in the development of novel bioactive molecules. Recent studies have explored its role as a building block for the synthesis of heterocyclic compounds, its interactions with biological targets, and its potential as a lead compound for drug discovery.

A 2023 study published in the Journal of Medicinal Chemistry investigated the use of Formamide,N-(2-bromophenyl)- as a precursor for the synthesis of benzimidazole derivatives with potent kinase inhibitory activity. The researchers demonstrated that the bromine atom at the 2-position of the phenyl ring significantly influenced the binding affinity of the resulting compounds to various kinase targets, particularly those involved in cancer signaling pathways. The study reported several derivatives with IC50 values in the low nanomolar range against specific oncogenic kinases, highlighting the importance of this structural motif in medicinal chemistry.

In the field of chemical biology, a recent breakthrough (Nature Chemical Biology, 2024) revealed that Formamide,N-(2-bromophenyl)- can serve as a covalent modifier of cysteine residues in proteins. The electrophilic nature of the bromine atom allows for selective modification of target proteins, enabling the development of new chemical probes for studying protein function. This property has been exploited in activity-based protein profiling (ABPP) studies, providing insights into previously undruggable targets.

From a synthetic chemistry perspective, advances in catalytic systems have improved the efficiency of reactions involving Formamide,N-(2-bromophenyl)-. A 2024 publication in ACS Catalysis reported a palladium-catalyzed cross-coupling protocol that significantly enhances the yield of N-aryl formamide derivatives while maintaining excellent functional group tolerance. This methodological improvement has facilitated the synthesis of diverse compound libraries for high-throughput screening in drug discovery programs.

The pharmaceutical potential of Formamide,N-(2-bromophenyl)- derivatives has been further demonstrated in recent preclinical studies. A series of compounds derived from this scaffold have shown promising activity against resistant bacterial strains, with one candidate currently in Phase I clinical trials for the treatment of multidrug-resistant tuberculosis. The unique electronic properties imparted by the bromine substitution appear to contribute to both the antimicrobial activity and the ability to evade common resistance mechanisms.

Looking forward, researchers are particularly excited about the application of Formamide,N-(2-bromophenyl)- in targeted protein degradation strategies. Preliminary data presented at the 2024 American Chemical Society National Meeting suggests that derivatives of this compound can be engineered to serve as effective E3 ligase recruiters in PROTAC (Proteolysis Targeting Chimera) molecules. This approach could open new avenues for the treatment of diseases traditionally considered undruggable by small molecules.

In conclusion, Formamide,N-(2-bromophenyl)- (CAS: 10113-38-9) continues to emerge as a valuable scaffold in chemical biology and drug discovery. Recent studies have expanded our understanding of its synthetic utility, biological interactions, and therapeutic potential. As research progresses, we anticipate seeing more applications of this versatile compound in addressing challenging biological targets and developing novel therapeutic agents.

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