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- W2044283603 abstract "2‘,3‘-Dideoxy-5-fluoro-3‘-thiacytidine [(−)-FTC], the active ingredient in the antiviral drug emtricitabine (Emtriva), was prepared by a bioresolution process using cholesterol esterase immobilized on Accurel PP to resolve optical isomers of racemic FTC butyrate. Cholesterol esterase was immobilized at 1.9-kg scale. Recycling studies were carried out with racemic FTC butyrate that indicated a high degree of immobilized cholesterol esterase stability resulting in 15 successive cycles of use (14 recycles). Racemic FTC butyrate (∼8 kg, 200 g/L) was resolved with immobilized cholesterol esterase using a 1-pentanol/ potassium dihydrogen phosphate buffer−solvent system to give (−)-FTC·HCl (98% ee, 2.17 kg, 31% molar yield based on racemic FTC butyrate)." @default.
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- W2044283603 date "2006-03-23" @default.
- W2044283603 modified "2023-10-10" @default.
- W2044283603 title "Immobilization of Cholesterol Esterase for Use in Multiple Batch Biotransformations to Prepare (−)- FTC (Emtricitabine)" @default.
- W2044283603 cites W1975793843 @default.
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- W2044283603 doi "https://doi.org/10.1021/op050258f" @default.
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