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A Single-Step Synthesis of Azetidine-3-Amines

preprint
submitted on 22.08.2020 and posted on 24.08.2020 by Brian J Wang, Matthew Duncton

The azetidine group is frequently encountered within contemporary medicinal chemistry where it is viewed as a privileged structure. However, the introduction of an azetidine can be synthetically challenging. Herein, a straight-forward one step synthesis of azetidine-3-amines, starting from a bench stable, commercial material is presented. The reaction tolerates functional groups commonly encountered in biological-, medicinal- and agro-chemistry, and proceeds in moderate-to-high yield with secondary amines, and moderate-to-low yield with primary amines. The methodology compares favorably to recent alternative procedures and can be utilized in “any-stage” functionalization, including late-stage azetidinylation of approved drugs and other compounds with pharmacological activity.

History

Email Address of Submitting Author

matt@dunctonllc.com

Institution

Duncton, LLC

Country

United States

ORCID For Submitting Author

0000-0002-6007-7515

Declaration of Conflict of Interest

The author declare no conflicts of interest

Version Notes

Version 1 - submitted manuscript

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