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CAS No. 2738675-96-0, Benzonitrile, 3-[[(3R)-2,3-dihydro-3-hydroxy-7-(methylsulfonyl)-1-oxo-1H-inden-4-yl]oxy]-5-fluoro-

  • 2738675-96-0

  • C17H12FNO5S

  • 361.34

  • 1.56±0.1

  • 98% min (HPLC)

  • von Hippel-Lindau (VHL) disease-associated cancers

  • Belzutifan

  • 9/5/2034 (Belzutifan)

  • HIF-2α (EPAS1)

  • N

  • 2023

  • ISO 9001;ISO 14001;ISO 45001

Availability:

Product Description

This product, CAS No. 2738675-96-0, is an N-3 intermediate for the synthesis of Belzutifan.


Belzutifan ROS main

Main ROS for Belzutifan. Key Belzutifan intermediates are boxed in blue.



References

Hamal, K. B. et al. Synthesis of the Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitor, 3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977, Belzutifan); Efficient Replication of Established Approaches. Tetrahedron Letters 128, 154691 (2023).
 


DiRocco, D. A. et al. Novel synthetic pathway to belzutifan. (2024).

 

Pirnot, M. et al. Manufacturing Process Development for Belzutifan, Part 6: Ensuring Scalability for a Deoxyfluorination Reaction. Org. Process Res. Dev. 26, 551–559 (2022).
 

Wang, T. et al. Manufacturing Process Development for Belzutifan, Part 5: A Streamlined Fluorination–Dynamic Kinetic Resolution Process. Org. Process Res. Dev. 26, 543–550 (2022).
 

Chen, Z. et al. Manufacturing Process Development for Belzutifan, Part 3: Completing a Streamlined Through-Process with a Safe and Scalable Oxidation. Org. Process Res. Dev. 26, 525–532 (2022).
 

Bottecchia, C. et al. Manufacturing Process Development for Belzutifan, Part 2: A Continuous Flow Visible-Light-Induced Benzylic Bromination. Org. Process Res. Dev. 26, 516–524 (2022).
 

BRUICK, R. K., CHEN, Y. & RUIZ, J. C. F. HIF-2α INHIBITORS FOR TREATING IRON OVERLOAD DISORDERS. (2016).
 

Wehn, P. M. et al. Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S )-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H -inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385). J. Med. Chem. 61, 9691–9721 (2018).
 

Josey, J. A., Wallace, E. M., Du, X. & GOGGIN, B. Compositions for use in treating pulmonary arterial hypertension. (2016).
 

Ji, Y. et al. Benzylic Photobromination for the Synthesis of Belzutifan: Elucidation of Reaction Mechanisms Using In Situ LED-NMR. J. Org. Chem. 87, 2055–2062 (2022).
 

薛晓纤 et al. 一种Belzutifan的中间体的制备方法. (2023).
 

Yang, F., Yu, N., CHI, J., He, F. & Tao, W. 6-oxo-1,6-dihydropyridazine derivative, preparation method therefor and medical use thereof. (2021).
 

Xu, R. et al. 3-[(1 S ,2 S ,3 R )-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma. J. Med. Chem. 62, 6876–6893 (2019).


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