Efficient Synthesis of 3-R-Boc-amino-4-(2,4,5-trifluorophenyl)butyric Acid |
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Authors: | Xianhua Pan Shupei Bai Wansheng Yu Ding Ding Dongxian Zhao |
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Institution: | Shanghai Institute of Technology, Shanghai, China |
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Abstract: | 3-R-Boc-amino-4-(2,4,5-trifluorophenyl)butyric acid (9) was obtained from L-methionine in six steps with a total yield of 32%. The α-amino acid segment of L-methionine was transferred to chiral aziridine by amino protection, reduction, hydroxyl derivation, and cyclization. After ring opening of 2,4,5-trifluoro-phenyl magnesium bromide, the methylthiomethyl group was then hydrolyzed to β-amino alcohol and oxidized to the target β-amino acid. |
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Keywords: | β-Amino acid" target="_blank">β-Amino acid aziridine Grignard reaction hydrolyze methylthiomethyl |
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