An improved and scalable process for 3,8-diazabicyclo[3.2.1]-octane analogues |
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Authors: | Long Jiang Huang Da Wei Teng College of Chemical Engineering Qingdao University of Science & Technology Qingdao China |
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Institution: | 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-diazabicyclo3.2.1]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- diazabicyclo3.2.1]octane analogue 12 was obtained in a total yield of 42%in five steps. |
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Keywords: | 3 8-Diazabicyclo[3 2 1]octane:Scaffold Process development |
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