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ChemicalBook CAS DataBase List Bosentan
147536-97-8

Bosentan synthesis

7synthesis methods
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.
Synthetic Routes
  • ROUTE 1

    • 202112075109695574.jpg

    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

  • ROUTE 2

    • 202112070211989451.jpg

    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

  • ROUTE 3

    • 202112076962480783.jpg

    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

  • ROUTE 4

    • 202112073818854112.jpg

    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

  • ROUTE 5

    • 202112078848886444.jpg

    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

  • ROUTE 6

    • 202112079350012532.jpg

    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

  • ROUTE 7

    • 202112072927216959.jpg

    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

  • ROUTE 8

    • 202112076700757683.jpg

    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

  • ROUTE 9

    • 202112077584711962.jpg

    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

  • ROUTE 10

    • 202112075770859426.jpg

    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

202112075109695574.jpg

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

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Yield:147536-97-8 95.7%

Reaction Conditions:

Stage #1: ethylene glycol;4-tert-butyl-N-(6-chloro-5-(2-methoxyphenoxy)2,2'-bipyrimidin-4-yl)benzene sulfonamidewith sodium hydroxide in tetrahydrofuran at 60 - 65; for 12 h;
Stage #2: with tartaric acid in tetrahydrofuran;water at 5 - 10; for 1 h;

Steps:

8

Example 8: Preparation of crude Bosentan from compound of formula Via.The compound of formula Via (130.0g, 1.0eq), ethylene glycol (1470.0ml,107.0eq) and sodium hydroxide (88.9g, 9.0eq) were heated in tetrahydrofuran (1560.0ml,12.0vol) at 60- 65°C for 12hours. After completion of reaction, the reaction mixture was added to a mixture of water (4450.0ml,35.0vol) and DL-Tartaric acid (185.0g, 5.0eq) at 5-10°C. Maintained at this temperature for 1 hour. Filtered the solid and washed with water (1300.0ml). Dried the solid, Bosentan, under vacuum at 50-55°C for 12 hours to get the title compound (Yield: 134.5g (95.7%, HPLC purity 98.41 %).

References:

WO2012/56468,2012,A1 Location in patent:Page/Page column 16

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