Enantioselective synthesis of a key intermediate of Levofloxacin using microbial resolution |
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| Affiliation: | 1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;2. Laboratory of Biology, School of Higher Vocational Education, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, PR China;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey;2. Department of Biochemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey;1. Heinrich Heine University Duesseldorf, Institute of Pharmaceutical and Medicinal Chemistry, Universitaetstr. 1, 40225 Duesseldorf, Germany;2. Laboratory of Medicinal Chemistry (IQOG, CSIC), C/ Juan de la Cierva 3, 28006, Madrid, Spain;1. Discovery Pharmaceutical Sciences, MRL, Merck & Co., Inc., West Point, PA 19486, USA;2. Discovery Chemistry, MRL, Merck & Co., Inc., West Point, PA 19486, USA |
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| Abstract: | The important key intermediate in the synthesis of Levofloxacin, (S)-7,8-difluoro-2,3-dihydro-3-methyl-4H-1,4-benzoxazine, was prepared enantioselectively by microbial resolution. When lyophilized microorganism selected from soil was treated with the corresponding amide, the (S)-amine was obtained with high enantiomeric purity (99% ee). |
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