SUCCINCT SYNTHESIS OF BOSENTAN UTILIZING GLYCOL MONO-THP ETHERopen access
- Authors
- Lee, Chung Ryul; Lee, Sang Yeul; Nam, Tae-gyu
- Issue Date
- Jul-2014
- Publisher
- TAYLOR & FRANCIS INC
- Keywords
- Bosentan; endothelin receptor antagonist; pulmonary arterial hypertension; tetrahydropyran ether
- Citation
- SYNTHETIC COMMUNICATIONS, v.44, no.17, pp.2488 - 2493
- Indexed
- SCIE
SCOPUS
- Journal Title
- SYNTHETIC COMMUNICATIONS
- Volume
- 44
- Number
- 17
- Start Page
- 2488
- End Page
- 2493
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/25902
- DOI
- 10.1080/00397911.2014.904881
- ISSN
- 0039-7911
- Abstract
- A concise synthetic method for bosentan, a nonpeptide orally active dual endothelin (ET-1(A/B)) receptor antagonist used for the treatment of pulmonary artery hypertension (PAH), was developed. We developed a new succinct synthetic route for bosentan by employing an acid-labile tetrahydropyran (THP)-protected glycol. THP group is advantageous over the previously known protection groups used in bosentan synthesis in that it provides a clean and quantitative deprotection. Bosentan was constructed via two parallel reaction pathways, yet the better product yield was obtained from a pathway via 6. Deprotection of THP ether was achieved under a mild acidic condition to afford bosentan.
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