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ChemicalBook CAS DataBase List Tenofovir Alafenamide
379270-37-8

Tenofovir Alafenamide synthesis

2synthesis methods
Tenofovir alafenamide, also known as TAF and GS-7340, is a nucleotide reverse transcriptase inhibitor (NRTIs) and a novel prodrug of tenofovir. By blocking reverse transcriptase, TAF prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug, which means that it is an inactive drug. In the body, tenofovir alafenamide is converted to tenofovir diphosphate (TFV-DP). Tenofovir alafenamide fumarate was approved in November 2015 for treatment of HIV-1. Synthetic Description Reference: Zhang, Wei; Liao, Wensheng. Method for preparing tenofovir alafenamide Zhang, Wei; Liao, Wensheng. CN 108623632. (Shanghai Steppharm Co., Ltd., Peop. Rep. China) Synthetic Description Reference: Zhong, Bohua; Wang, Jianming; Jin, Xuefeng. Single isomer of phosphoric acid/phosphonic acid derivative and its medical application. CN 108129514. (Beijing Meibeita Pharmaceutical Research Co., Ltd., Peop. Rep. China) Synthetic Description Reference: Wang, Jianming; Chen, Xiaoguang; Chen, Junping; Fan, Shan. Phosphoric acid/phosphonic acid derivatives and medicinal uses thereof. WO 2014183462. (Beijing Meibeita Drug Res Co., Ltd, Peop. Rep. China) Synthetic Description Reference: Wei, Yonggang; Qiu, Guanpeng; Lu, Yonghua; Zhu, Guozhi. Method for preparing nucleoside analogue and intermediate thereof. WO 2015161781. (Sichuan Haisco Pharmaceutical Co., Ltd., Peop. Rep. China)
Synthetic Routes
  • ROUTE 1
  • 202112072228068427.jpg

    Reference: Zhang, Wei; Liao, Wensheng. Method for preparing tenofovir alafenamide Zhang, Wei; Liao, Wensheng. CN 108623632. (Shanghai Steppharm Co., Ltd., Peop. Rep. China)

  • ROUTE 2
  • 202112076167835962.jpg

    Reference: Zhong, Bohua; Wang, Jianming; Jin, Xuefeng. Single isomer of phosphoric acid/phosphonic acid derivative and its medical application. CN 108129514. (Beijing Meibeita Pharmaceutical Research Co., Ltd., Peop. Rep. China)

  • ROUTE 3
  • 202112079963497397.jpg

    Reference: Wang, Jianming; Chen, Xiaoguang; Chen, Junping; Fan, Shan. Phosphoric acid/phosphonic acid derivatives and medicinal uses thereof. WO 2014183462. (Beijing Meibeita Drug Res Co., Ltd, Peop. Rep. China)

  • ROUTE 4
  • 202112076782665535.jpg

    Reference: Wei, Yonggang; Qiu, Guanpeng; Lu, Yonghua; Zhu, Guozhi. Method for preparing nucleoside analogue and intermediate thereof. WO 2015161781. (Sichuan Haisco Pharmaceutical Co., Ltd., Peop. Rep. China)

  • ROUTE 5
  • 202112070170065071.jpg

    Chapman, H.; Kernan, M.; Prisbe, E.; Rohloff, J.; Sparacino, M.; Terhorst, T.; Yu, R. Practical synthesis, separation, and stereochemical assignment of the PMPA pro-drug GS-7340. Nucleosides, Nucleotides & Nucleic Acids. Volume 20. Issue 4-7. Pages 621-628. 2001.

  • ROUTE 6
  • 202112076643214341.jpg

    Becker, Mark W.; Chapman, Harlan H.; Cihlar, Tomas; Eisenberg, Eugene J.; He, Gong-Xin; Kernan, Michael R.; Lee, William A.; Prisbe, Ernest J.; Rohloff, John C.; Sparacino, Mark L. Preparation of prodrugs amino acid methoxyphosphonate acyclic nucleotide analogs as antiviral or antitumor agents and their use in therapy and prophylaxis. Assignee Gilead Sciences, Inc., USA. WO 2002008241 A2. (2002).

  • ROUTE 7
  • 202112073214049923.jpg

    Vellanki, Siva Ram Prasad; Balusu, Raja Babu; Putta, Subba Rayudu; Raavi, Mastan Rao; Arikatla, Sivalakshmi Devi. Process for the preparation of tenofovir alafenamide and its pharmaceutically acceptable salts. Assignee Mylan Laboratories Ltd., India. IN 2014MU00118 A. (2015).

  • ROUTE 8
  • 202112072706788664.jpg

    Thatipally, Suresh; Dammalapati, Venkata Lakshmi Narasimha Rao; Kallam, Venkata Siva Ramakrishna Reddy; Gorantla, Seeta Rama Anjaneyulu; Chava, Satyanarayana. An improved process for the preparation of tenofovir alafenamide via separation of its diastereomers by simulated moving chromatography and its pharmaceutically acceptable salts. Assignee Laurus Labs Private Limited, India. WO 2015040640 A2. (2015).

202112072228068427.jpg

Reference: Zhang, Wei; Liao, Wensheng. Method for preparing tenofovir alafenamide Zhang, Wei; Liao, Wensheng. CN 108623632. (Shanghai Steppharm Co., Ltd., Peop. Rep. China)

39825-33-7 Synthesis
L-Alanine Isopropyl Ester

39825-33-7
235 suppliers
$14.00/25g

379270-35-6 Synthesis
phenyl hydrogen ((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonate

379270-35-6
184 suppliers
inquiry

Tenofovir Related Compound 6

383365-04-6
52 suppliers
inquiry

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39825-33-7 Synthesis
L-Alanine Isopropyl Ester

39825-33-7
235 suppliers
$14.00/25g

379270-35-6 Synthesis
phenyl hydrogen ((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonate

379270-35-6
184 suppliers
inquiry

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