Bosentan

CAT#: H317331

CAS#: 147536-97-8

Description: Bosentan is a mixed Endothelin Receptor Antagonist which is used as a vasodilator. Bosentan is an inhibitor of ETAR and ETBR. It is used for the treatment of pulmonary artery hypertension (PAH). Bosentan blocks the action of endothelin molecules that would otherwise promote narrowing of the blood vessels and lead to high blood pressure.

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Synthetic Routes

Bosentan - Synthetic Route 1

Bosentan route01

Synthetic reference

Raju, K. Rajasekhara; Reddy, B. Shankar; Somannavar, Y. S.; Sinha, B. K.; Babu, P. N. Kishore; Raju, K. Mohana. Improved Large-Scale Synthesis of Bosentan Monohydrate. Organic Preparations and Procedures International. Chemical Research and Development. Aurobindo Pharma Ltd. Telangana, India. Volume 48. Issue 6. Pages 481-491. 2016

Bosentan - Synthetic Route 2

Bosentan route02

Synthetic reference

Gudekar, Sanket; Lokhande, Rama; Sutar, Rajiv; Pednekar, Sanjay; Surve, Sandip; Kolhal, Surekha. Synthesis and characterisation of process related impurity in Bosentan Monohydrate. Journal of Chemical and Pharmaceutical Research. School of Basic Sciences, Department of Chemistry. Jaipur National University. Jaipur, India. Volume 5. Issue 11. Pages 600-604, 5 pp.2013

Bosentan - Synthetic Route 3

Bosentan route03

Synthetic reference

Rebelli, Pradeep; Yerrabelly, Jayaprakash Rao; Yalamanchili, Bharathi kumari; Kommera, Rajashekar; Ghojala, Venkat Reddy; Bairy, Kondal Reddy. New approaches to endothelin receptor antagonist – bosentan. Letters in Organic Chemistry. Department of Research and Development. MSN R and D centre. Medak, Andhra Pradesh, India 502307. Volume 10. Issue 5. Pages 364-368. 2013

Bosentan - Synthetic Route 4

Bosentan route04

Synthetic reference

Lee, Chung Ryul; Lee, Sang Yeul; Nam, Tae-gyu. Succinct Synthesis of Bosentan Utilizing Glycol Mono-THP Ether. Synthetic Communications. Department of Pharmacy and Institute of Pharmaceutical Science and Technology. Hanyang University. Gyeonggi-do, S. Korea. Volume 44. Issue 17. Pages 2488-2493. 2014

Bosentan - Synthetic Route 5

Bosentan route05

Synthetic reference

Harrington, Peter J.; Khatri, Hiralal N.; DeHoff, Brad S.; Guinn, Martin R.; Boehler, Mark A.; Glaser, Karl A. Research and Development of a Second-Generation Process for Bosentan, an Endothelin Receptor Antagonist. Organic Process Research & Development. Boulder Technology Center. Roche Colorado Corporation. Boulder, USA 80301. Volume 6. Issue 2. Pages 120-124. 2002

Bosentan - Synthetic Route 6

Bosentan route06

Synthetic reference

Bolli, Martin H.; Boss, Christoph; Binkert, Christoph; Buchmann, Stephan; Bur, Daniel; Hess, Patrick; Iglarz, Marc; Meyer, Solange; Rein, Josiane; Rey, Markus; Treiber, Alexander; Clozel, Martine; Fischli, Walter; Weller, Thomas. The Discovery of N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist. Journal of Medicinal Chemistry. Drug Discovery Chemistry. Actelion Pharmaceuticals Ltd.. Allschwil, Switz. CH-4123.Volume 55 Issue 17. Pages 7849-7861. 2012

Bosentan - Synthetic Route 7

Bosentan route07

Synthetic reference

Yang, Ning; Dong, Junjun; Liu, Keliang. Synthesis of bosentan as an endothelin receptor antagonist. Zhongguo Yaowu Huaxue Zazhi. Institute of Pharmacology and Toxicology. Academy of Military Medical Sciences. Beijing, Peop. Rep. China 100850. Volume 15. Issue 4. Pages 230-233. 2005

Bosentan - Synthetic Route 8

Bosentan route08

Synthetic reference

Yang, Yi-hong; Yin, Di; Zhang, Heng. On synthesis of bosentan. Wuhan Gongcheng Daxue Xuebao. Key Laboratory for Green Chemical Process of Ministry of Education. Wuhan Institute of Technology. Wuhan, Hubei Province, Peop. Rep. China 430074. Volume 34. Issue 12. Pages 1-3, 7 2012

Bosentan - Synthetic Route 9

Bosentan route09

Synthetic reference

Shimpi, Nitin; Jaware, Jalindar; Bijukumar, Gopinathan Pillai; Prabhavat, Manoj Devilalji; Nadkarni, Sunil Sadanand. Process for the preparation of bosentan. Assignee Torrent Pharmaceuticals Ltd., India. IN 2009MU01366. 2010

Bosentan - Synthetic Route 10

Bosentan route010

Synthetic reference

Gant, Thomas G.; Sarshar, Sepehr. Substituted pyrimidines as endothelin modulators and their preparation and use in the treatment of diseases. Assignee Auspex Pharmaceuticals, Inc., USA. US 20080242687. 2008