Scalable Synthesis of 4-Bromo-1,2-dimethyl-1H-imidazole

Cost-Effective and Scalable Synthesis of 4-Bromo-1,2-dimethyl-1H-imidazole: A Key Building Block for Bioactive Molecules: M. Vetrichelvan, V. Lanke, B. Chandu, A. Mathur, A. Gupta
SynOpen 2023, 7, 496–500

4-Bromo-1,2-dimethyl-1H-imidazole is an important building block for the synthesis of a wide range of active pharmaceutical ingredients, and a useful starting material in medicinal chemistry. Commercial availability of large quantities of the title compound is neither ideal nor reliable, furthermore its preparation on a large scale by means of known methods is challenging for several reasons, including the formation of mixtures of regioisomers and modest yields. Recently, the group of Dr. Muthalagu Vetrichelvan from the Biocon Bristol Myers Squibb R&D Centre (Bangalore, India) reported a more efficient and scalable synthesis of 4-bromo-1,2-dimethyl-1H-imidazole, which under optimized conditions can be performed on a 100 g to 1 kg scale in about 92% isolated yield.

Dr. Vetrichelvan said: “We have reported a cost-effective, scalable, high-yielding, and commercially viable synthesis of 4-bromo-1,2-dimethyl-1H-imidazole, which is a key building block to construct various bioactive compounds.” 

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