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New strategy for the synthesis of phosphatase inhibitors TMC-69-6H and analogs |
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| Authors: | Nicolas Brondel Brigitte Renoux Jean-Pierre Gesson |
| Affiliation: | aLaboratoire ‘Synthèse et Réactivité des Substances Naturelles’, UMR CNRS 6514 40, Avenue du Recteur Pineau, F-86022 Poitiers Cedex, France |
| Abstract: | An efficient method for the synthesis of antitumor TMC-69-6H and related analogs which have been demonstrated to be phosphatase (PTP1B, VHR, and PP1) inhibitors, is reported. This strategy involves two key steps: a diastereoselective aldol reaction and a one-pot tandem ring-closing and cross metathesis for the construction of the pyran moiety. |
| Keywords: | TMC-69-6H Antitumor activity PTP1B inhibitor Diastereoselective aldolization Metathesis |
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