Concise enantioselective synthesis of duloxetine via direct catalytic asymmetric aldol reaction of thioamide |
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Authors: | Suzuki Yuta Iwata Mitsutaka Yazaki Ryo Kumagai Naoya Shibasaki Masakatsu |
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Affiliation: | Institute of Microbial Chemistry, Tokyo, 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan. |
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Abstract: | Direct catalytic asymmetric aldol reaction of thioamide offers a new entry to the concise enantioselective synthesis of duloxetine. The direct aldol protocol was scalable (>20 g) to afford the aldol product in 92% ee after LiAlH(4) reduction, and 84% of the chiral ligand was recovered after recrystallization. The following four steps of transformation delivered duloxetine. |
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