Organic Process Research & Development · 2011 · 12 citations · 7 references
PharmacyMedicinal ChemistryPharmacologyBiocatalysisDrug DiscoveryEnzymologyChemoenzymatic SynthesisEnzymatic CatalysisPotency OptimizationBromine Radical ChemistryCatalytic AcylationChemoenzymatic Asymmetric SynthesisChiral Product SynthesisEnantioselective SynthesisFriedel-crafts AcylationKetoreductase CatalysisSelective Acylation
This communication describes proof of concept for an enantioselective enzyme-based synthesis of diarylmethanol ( S )- 1 to access mGlu2 receptor potentiators. A ketoreductase (KRED) screen was applied to benzophenone 8 to afford chiral diarylmethanol ( S )- 9, which is a useful intermediate for the preparation of chiral diarylmethanol ( S )- 1 . In addition, a more practical synthesis of benzophenone 8 was demonstrated utilizing Friedel–Crafts acylation and radical bromination chemistry.
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David R. Helton, J P Tizzano, James A. Monn et al. · Journal of Pharmacology and Experimental Therapeutics · 1998 · 282 citations
Medicine, Neuroscience, Pharmacology +15