Total synthesis of BE-43547A2 |
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| Authors: | Yuanjun Sun Xiuwen Su Ruifei Zhou Dehong Wang Yuan Zhao Yuhang Jiang Liang Wang Yue Chen |
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| Affiliation: | 1. The State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, 300350, PR China;2. Collaborative Innovation Center of Chemical Science and Engineering, Tianjin, PR China |
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| Abstract: | An asymmetric total synthesis of BE-43547A2 has been achieved in 16 steps (longest linear) on a 3.2 gram scale. The details of our efforts that led to the total synthesis of BE-43547A2 were reported, the final 6 steps were optimized, and the overall yield was improved from 4.5% to 9.7%. The procedure utilized in the final 2 steps may serve as a better method for separating unstable APD compounds. |
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| Keywords: | Total synthesis BE-43547 α-Hydroxylation Hypoxia-selective Pancreatic cancer |
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