Improved synthesis of rupintrivir

Daizong Lin, Wangke Qian, Rolf Hilgenfeld, Hualiang Jiang, Kaixian Chen, Hong Liu*

*Corresponding author for this work

Abstract

An improved synthesis of rupintrivir (AG7088) was accomplished using three amino acids (l-glutamic acid, d-4-fluorophenylalanine, and l-valine) as the building blocks. The key fragment ketomethylene dipeptide isostere was constructed with the valine derivative and phenylpropionic acid derivative, followed by coupling with a lactam derivative and an isoxazole acid chloride to provide AG7088 totally in eight steps.

Original languageEnglish
JournalScience China Chemistry
Volume55
Issue number6
Pages (from-to)1101-1107
Number of pages7
ISSN1674-7291
DOIs
Publication statusPublished - 01.06.2012

Funding

We gratefully acknowledge financial support from the National Natural Science Foundation of China (20872153, 21021063, 20720102040 and 81025017), the National Basic Research Program of China grant (2009CB918502), the Chinese Academy of Sciences (XDA01040305), and the SILVER project of the European Commission (contract HEALTH-F3-2010-260644). HR is supported by a Chinese Academy of Sciences Visiting Professorship for Senior International Scientists (2010T1S6).

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

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