Tamiflu is one of the most effective anti-influenza drugs, which is currently manufactured by Hoffmann-La Roche from shikimic acid. Owing to its importance, more than 60 synthetic routes have been developed to date, however most of the synthetic routes utilise the potentially hazardous azide chemistry making them not green, thus not amenable to easy scale up. Consequently, this study exclusively demonstrated safe and efficient handling of potentially explosive azide chemistry involved in a proposed Tamiflu route by taking advantage of the continuous flow technology. The azide intermediates were safely synthesised in full conversions and >89 % isolated yields.
Keywords: azide chemistry; continuous flow synthesis; hazardous; safe; Tamiflu
When a peer-reviewed version of this preprint is available in the Beilstein Journals, this information will be updated in the information box above. If no peer-reviewed version is available, please cite this preprint using the following information:
Sagandira, C.; Watts, P. Beilstein Arch. 2019, 201984. doi:10.3762/bxiv.2019.84.v1
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