Base Information
- Chemical Name:2-BroMo-3-fluoroanisole
- CAS No.:46-59-3
- Molecular Formula:C7H6BrFO
- Molecular Weight:205.0243432
- Hs Code.:
- Mol file:46-59-3.mol
Synonyms:
Synonyms:
The study presents a novel and efficient synthetic process for bosentan monohydrate, an endothelin receptor antagonist used to treat pulmonary hypertension. The key innovation involves coupling p-tert-butyl-N-(6-chloro-5-(2-methoxy phenoxy)-2,2'-bipyrimidin-4-yl)benzenesulfonamide (7) with (2,2-dimethyl-1,3-dioxolane-4,5-diyl)dimethanol (14). This method eliminates the formation of critical impurities such as pyrimidinone 8, dimer impurity 9, and N-alkylated impurity 13, which are common in previous synthesis methods. The new process achieves an overall yield of 50-55%, corresponding to an average step yield of 85%, using simple steps and commercially available chemicals. The study also details the optimization of reaction conditions, such as the use of acetonitrile as a solvent and NaOH as a base, and the final purification of bosentan monohydrate using a combination of ethylacetate and methanol. The resulting bosentan monohydrate meets ICH-grade quality standards and exhibits polymorphic stability under various conditions.
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