Product Details

5-(4-Bromophenyl)-4,6-dichloropyrimidine (CAS 146533-41-7) is a halogenated diaryl pyrimidine of the bromophenyl-dichloropyrimidine chemical class. This compound is a key early-stage synthetic building block for making Macitentan, which is a dual endothelin receptor antagonist for pulmonary arterial hypertension (PAH). The aryl bromide at the para-position of the phenyl ring is good for Pd-catalyzed cross-coupling (Suzuki, Miyaura) to add more detail, but this position stays in the final API when making Macitentan. The reactive dichloropyrimidine scaffold has many electrophilic sites. The selectivity of SNAr is determined by the reaction conditions and electronic activation. As a reactive intermediate with ICH M7 aromatic halide genotoxic alert potential, it is very important to keep track of impurities from this point on. 

ApiSyn sells 5-(4-Bromophenyl)-4,6-dichloropyrimidine (CAS 146533-41-7) as a pharmaceutical synthetic intermediate and reference standard for the development of Macitentan and other endothelin receptor antagonists.