Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/150792
Title: Generation of a heteropolycyclic and sp3-rich scaffold for library synthesis from a highly diastereoselective Petasis/Diels–Alder and ROM–RCM reaction sequence
Authors: Flagstad, Thomas
Azevedo, Carlos M. G.
Troelsen, Nikolaj S.
Min, Geanna K.
Macé, Yohan
Willaume, Anthony
Guilleux, Rachel
Velay, Mélanie
Bonnet, Karine
Morgentin, Remy
Nielsen, Thomas E.
Clausen, Mads H.
Keywords: Science::Chemistry
Issue Date: 2019
Source: Flagstad, T., Azevedo, C. M. G., Troelsen, N. S., Min, G. K., Macé, Y., Willaume, A., Guilleux, R., Velay, M., Bonnet, K., Morgentin, R., Nielsen, T. E. & Clausen, M. H. (2019). Generation of a heteropolycyclic and sp3-rich scaffold for library synthesis from a highly diastereoselective Petasis/Diels–Alder and ROM–RCM reaction sequence. European Journal of Organic Chemistry, 2019(5), 1061-1076. https://dx.doi.org/10.1002/ejoc.201801551
Journal: European Journal of Organic Chemistry
Abstract: Efficient access to diverse screening compounds with desirable, lead-like properties can be a bottleneck in early drug discovery and chemical biology. Herein we present an efficient, rapid route to three structurally distinct classes of compounds (A–C) from a single precursor, which in turn is available through a one-pot Petasis 3-component reaction/Diels–Alder cascade reaction. We demonstrate the versatility of the approach through the synthesis of 35 exemplary compounds from the three classes, as well as by the production of 2188 final compounds, which have been included in the Joint European Compound Library of the European Lead Factory.
URI: https://hdl.handle.net/10356/150792
ISSN: 1434-193X
DOI: 10.1002/ejoc.201801551
Rights: © 2019 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. All rights reserved.
Fulltext Permission: none
Fulltext Availability: No Fulltext
Appears in Collections:SCELSE Journal Articles

Page view(s)

86
Updated on Jan 23, 2022

Google ScholarTM

Check

Altmetric


Plumx

Items in DR-NTU are protected by copyright, with all rights reserved, unless otherwise indicated.