Events8th International Electronic Conference on Medicinal Chemistry
Event submissions
Published
with-doi10.3390/ECMC2022-13471
This submission belongs to the session S4. Small molecules as drug candidates of the event 8th International Electronic Conference on Medicinal Chemistry
Published date
01 Nov, 2022
Academic Editor
author-avatarAlfredo Berzal-Herranz
Citation
Linda Supe, Synthesis of azetidine-based beta-amino alcohols, in Proceedings of 8th International Electronic Conference on Medicinal Chemistry, 1 November–30 November 2022, MDPI: Basel, Switzerland, doi: 10.3390/ECMC2022-13471
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Synthesis of azetidine-based beta-amino alcohols

Linda Supe 1
1. Latvian Institute of Organic Synthesis
Abstract

Beta-amino alcohols are versatile chemicals used as scaffolds in medicinal chemistry and are key factors for the efficacy of numerous pharmaceutical products. Locking the conformation of the active fragment in bioactive molecules may increase the potency and selectivity towards target receptor. Small rings especially the azetidine framework can serve as conformational lock yet providing the necessary size for receptor binding. Herein we report the synthesis of enantiopure beta-amino alcohols where the motif is combined with a structurally constrained azetidine cycle. The key steps towards target molecules include base-induced azetidine ring closure and subsequent beta-amino alcohol core installation.

Acknowledgements The research was funded by ERDF (Grant No. 1.1.1.2/VIAA/4/20/755)

Keywords
beta-amino alcohols
2,4-azetidines
2,2,4-azetidines
asymmetric synthesis
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