Hexafluoroisopropanol-Induced Facial Selectivity in a Hindered Diels–Alder Reaction
| Autor: | Florence F. Wagner, Brian T. Chamberlain, David J. P. Kornfilt, Isabelle Chataigner, Riccardo Spezia |
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| Rok vydání: | 2023 |
| Předmět: | |
| Zdroj: | Synthesis. |
| ISSN: | 1437-210X 0039-7881 |
| DOI: | 10.1055/a-2016-4548 |
| Popis: | BRD4780 is a small molecule that can selectively clear mutant MUC1-fs protein in mucin kidney disease models. Prior syntheses of BRD4780 were unsuitable for preparation on large scale. In this manuscript, HFIP is described as a unique solvent that allowed the key Diels–Alder reaction to proceed with >20:1 endo diastereoselectivity, enabling the kg-scale preparation of BRD4780 for further studies. |
| Databáze: | OpenAIRE |
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