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Published in 2019 at "ChemMedChem"
DOI: 10.1002/cmdc.201900398
Abstract: Although the advantages of sp3‐rich, sterically complicated molecules in drug development have been pointed out, modern screening libraries are filled with planar, sp2‐rich components. Compounds that are sp3‐rich are difficult to synthesize, and thus we…
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Keywords:
sp3;
lead identification;
lead like;
sp3 rich ... See more keywords
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Published in 2022 at "Organic letters"
DOI: 10.1021/acs.orglett.2c00228
Abstract: Reactions that require strictly dry conditions are challenging to translate to a DNA-encoded library format. Controlled pore glass solid support-connected DNA oligonucleotide-aldehyde conjugates could be condensed with SnAP reagents and cyclized to various sp3-rich heterocycles.…
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Keywords:
dna;
encoded library;
chemistry;
sp3 rich ... See more keywords
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Published in 2021 at "Chemical Science"
DOI: 10.1039/d1sc00161b
Abstract: Fragment-based drug discovery is an important and increasingly reliable technology for the delivery of clinical candidates. Notably, however, sp3-rich fragments are a largely untapped resource in molecular discovery, in part due to the lack of…
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Keywords:
methods modular;
synthetic methods;
sp3 rich;
emergent synthetic ... See more keywords
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Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc03009h
Abstract: By harnessing an energy transfer process, new photocatalyzed [2 + 2]-cycloadditions occurring between γ-alkylidene-γ-lactams and unsaturated substrates have been developed. The reaction mode is particularly powerful because it leads to the formation of different high…
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Keywords:
high value;
sp3 rich;
rich frameworks;
photocatalyzed cycloadditions ... See more keywords