【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
【机 构】
:
College of Chemical Engineering
论文部分内容阅读
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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