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Fit‐for‐Purpose Synthesis of CDK2 Inhibitor GNE‐140
A six‐step, stereoselective synthesis of cyclin‐dependent kinase 2 (CDK2) inhibitor GNE‐140 was developed. The key bonds were assembled through palladium‐catalyzed Negishi cross‐coupling and Buchwald–Hartwig C−N coupling steps. The stereodiad was established through a single‐step, CuH‐catalyzed enon...
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Published in: | Helvetica chimica acta 2023-08, Vol.106 (8), p.n/a |
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Main Authors: | , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | A six‐step, stereoselective synthesis of cyclin‐dependent kinase 2 (CDK2) inhibitor GNE‐140 was developed. The key bonds were assembled through palladium‐catalyzed Negishi cross‐coupling and Buchwald–Hartwig C−N coupling steps. The stereodiad was established through a single‐step, CuH‐catalyzed enone reduction proceeding in >99 : 1 er and 89 : 11 dr. GNE‐140 was obtained in 25 % overall yield with 98.6 A% HPLC purity. |
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ISSN: | 0018-019X 1522-2675 |
DOI: | 10.1002/hlca.202300023 |