Publication | Closed Access
The Development of a Large-Scale Synthesis of Matrix Metalloproteinase Inhibitor, ABT-518
11
Citations
5
References
2002
Year
Inhibitory ActivityMedicinal ChemistryMatrix Metalloproteinase InhibitorBioorganic ChemistryFirst Generation SynthesisBiochemistryNovel TherapyNatural SciencesMedicineMetalloproteinMolecular BiologyTitle CompoundDrug DevelopmentChemical BiologyPharmacologyLarge-scale SynthesisSix-step Synthetic SequenceDrug Discovery
A process for the preparation of matrix metalloproteinase inhibitor ABT-518 has been developed. Significant improvements have been made to the first generation synthesis and are described here. The new process is very robust and efficient; multikilogram quantities of the title compound have been synthesized for clinical trials. ABT-518 was prepared by this six-step synthetic sequence in 51% overall yield with >99% ee.
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