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Simple and Efficient Synthesis of Belinostat |
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| Authors: | Lei Yang Yihua Zhang |
| Institution: | 1. Department of Medicinal Chemistry , China Pharmaceutical University , Nanjing, China;2. Center of Drug Discovery , China Pharmaceutical University , Nanjing, China;3. Center of Drug Discovery , China Pharmaceutical University , Nanjing, China |
| Abstract: | A novel synthesis of belinostat (1) starting from 3-nitrobenzaldehyde has been developed. The key step in this sequence involves the conversion of (2E)-3-(3-aminophenyl)acrylic acid methyl ester to (2E)-3-(3-chlorosulfonylphenyl)acrylic acid methyl ester via diazotization and sulfonylation. |
| Keywords: | Belinostat sulfonylation synthesis |