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| An improved and scalable process for 3,8-diazabicyclo [3.2.1]-octane analogues |
| Long Jiang Huang, Da Wei Teng |
| College of Chemical Engineering, Qingdao University of Science & Technology, Qingdao 266042, China |
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Abstract An improved and scalable process for substituted 3,8-diazabicyclo [3.2.1]octane was developed.N-Benzyl-2,5-dicarbethoxy-pyrrolidine 2 was reduced to N-benzyl-2,5-dihydroxymethylpyrrolidine 9 and subsequently debenzylated to afford N-Boc-2,5-dihydroxymethylpyrrolidine 10.After mesylation of the diol 10 and cyclization with benzylamine, a diversity of scaffold, 3,8-diazabicyclo [3.2.1]octane analogue 12 was obtained in a total yield of 42% in five steps.
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Received: 23 August 2010
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| Fund:This research was partially supported by the program of research fund for returning scholars of Ministry of Education of China (No.200812053) |
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Corresponding Authors:
Da Wei Teng, E-mail address:dteng@qust.edu.cn
E-mail: dteng@qust.edu.cn
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Ming-Hua Chen, Sheng Lin, Ya-Nan Wang, Cheng-Gen Zhu, Yu-Huan Li, Jian-Dong Jiang, Jian-Gong Shi. Antiviral stereoisomers of 3,5-bis(2-hydroxybut-3-en-1-yl)-1,2, 4-thiadiazole from the roots of Isatis indigotica[J]. CCL, 2016, 27(05): 643-648. |
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