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 debenzylat...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.展开更多
基金supported by the program of research fund for returning scholars of Ministry of Education of China(No.200812053)
文摘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.
