Stereoselective synthesis of chiral β-amino trifluoromethyl alcohol: development of a manufacturing process for a key intermediate in the production of a novel elastase inhibitor,AE-3763 |
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Authors: | Yasunao Inoue Tomoki Omodani Ryotaro Shiratake Fuminori Sato |
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Institution: | Drug Research Division, Dainippon Sumitomo Pharma Co., Ltd, Enoki-cho 33-94, Suita, Osaka 564-0053, Japan |
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Abstract: | We have successfully synthesized chiral β-amino trifluoromethyl alcohol (2S,3S)-7a, which is a key intermediate in the production of AE-3763, by stereoselective reduction of N-Cbz-protected 5-hydroxy-5-(trifluoromethyl)-1,3-oxazolidine 4 prepared from L-valine in 3 steps followed by alkaline hydrolysis. This new method can be applied to the industrial-scale synthesis of AE-3763. |
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