Concise and efficient synthesis of eliglustat |
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| Authors: | Xiaoyu Liu Xiaoyu Li Hongguang Yang Xiang Shi Feilong Yang |
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| Affiliation: | State Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China |
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| Abstract: | Eliglustat, a ceramide glucosyltransferase inhibitor, was synthesized in six steps with 28.4% overall yield. The key features include the use of a diastereoselective aldol reaction to construct two contiguous stereocenters and a selective sulfonylation of a 1,3-diol catalyzed by dibutyltin oxide. |
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| Keywords: | Aldol reaction eliglustat selective sulfonylation stereogenic centers |
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