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Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities

✍ Scribed by Lin, Chien-Hung; Chang, Tsung-Che; Das, Anindya; Fang, Ming-Yu; Hung, Hui-Chen; Hsu, Kai-Cheng; Yang, Jinn-Moon; von Itzstein, Mark; Mong, Kwok Kong T.; Hsu, Tsu-An; Lin, Chun-Cheng


Book ID
120369420
Publisher
Royal Society of Chemistry
Year
2013
Tongue
English
Weight
718 KB
Volume
11
Category
Article
ISSN
1477-0520

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## Abstract The glucose‐, mannose‐, and galactose‐derived spirocyclic cyclopropylammonium chlorides **1a**–**1d, 2a**–**2d** and **3a**–**3d** were prepared as potential glycosidase inhibitors. Cyclopropanation of the diazirine **5** with ethyl acrylate led in 71% yield to a 4 : 5 : 1 : 20 mixture