Effective asymmetric synthesis of the key chiral building blocks of 20(S)- and 20(R)-camptothecins |
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Authors: | Sanbao Yu Xiangjun Feng Yu Luo Wei Lu |
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Affiliation: | (1) Department of Chemistry, East China Normal University, Shanghai, 200062, China;(2) Institute of Drug Discovery and Development, East China Normal University, Shanghai, 200062, China; |
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Abstract: | Abstract An effective diastereoselective synthesis of (S)-N,N-diethyl-2-formyl-2-(methoxymethoxy)butanamide and (S)-2-formyl-2-(methoxymethoxy)butanoic acid ethyl ester, which are two key chiral building blocks for the synthesis of 20(S)-camptothecins, has been developed by employing an asymmetric bromolactonization using (R)-proline. The (R) compounds were also synthesized to obtain 20(R)-camptothecin. |
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