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Unexpected Discovery of Saturated Pyridine Mimetics

06 February 2023, Version 1
Working Paper
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

A general approach to 3-azabicyclo[3.1.1]heptanes was unexpectedly discovered. The mechanism, scope, and scalability of this method were studied. The core was incorporated into the structure of the antihistamine drug Rupatidine instead of the pyridine ring, which led to a dramatic improvement in physicochemical properties.

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Version History

Feb 06, 2023 Version 1

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The content is available under CC BY 4.0 [opens in a new tab]

DOI

10.26434/chemrxiv-2023-jbb0r
D O I: 10.26434/chemrxiv-2023-jbb0r [opens in a new tab]

Funding

European Research Council (ERC)
101000893

Author’s competing interest statement

Authors are employees of a chemical supplier Enamine.

Ethics

The author(s) have declared ethics committee/IRB approval is not relevant to this content

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