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An Alternate Synthesis of Bosentan Monohydrate, an Endothelin Receptor Antagonist
- Source :
- Synlett. 25:265-269
- Publication Year :
- 2013
- Publisher :
- Georg Thieme Verlag KG, 2013.
-
Abstract
- An alternate synthesis of an endothelin receptor antagonist bosentan monohydrate is reported. This new synthetic route involves the coupling of p - tert -butyl- N -[6-chloro-5-(2-methoxy-phenoxy)(2,2′-bipyrimidin)-4-yl]benzene sulfonamide with commercially available raw material (2,2-dimethyl-1,3-dioxolan-4-yl)methanol as the key step. Attractive features of this approach are its versatileness, commercial availability of raw materials, usage of eco-friendly reagents, and it efficiently provides the desired bosentan monohydrate free from reported impurities such as dimer, N-alkylated, and pyrimidinone impurities.
Details
- ISSN :
- 14372096 and 09365214
- Volume :
- 25
- Database :
- OpenAIRE
- Journal :
- Synlett
- Accession number :
- edsair.doi...........0259db31ed395754862c08b7898b13fa