引用本文:
Long Jiang Huang, Da Wei Teng. An improved and scalable process for 3,8-diazabicyclo [3.2.1]-octane analogues[J]. Chinese Chemical Letters,
2011, 22(5): 523-526.
doi:
10.1016/j.cclet.2010.11.030
Citation: Long Jiang Huang, Da Wei Teng. An improved and scalable process for 3,8-diazabicyclo [3.2.1]-octane analogues[J]. Chinese Chemical Letters, 2011, 22(5): 523-526. doi: 10.1016/j.cclet.2010.11.030
Citation: Long Jiang Huang, Da Wei Teng. An improved and scalable process for 3,8-diazabicyclo [3.2.1]-octane analogues[J]. Chinese Chemical Letters, 2011, 22(5): 523-526. doi: 10.1016/j.cclet.2010.11.030
An improved and scalable process for 3,8-diazabicyclo [3.2.1]-octane analogues
摘要:
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.
English
An improved and scalable process for 3,8-diazabicyclo [3.2.1]-octane analogues
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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Key words:
- 3,8-Diazabicyclo[3.2.1]octane
- / Scaffold
- / Process development
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