Synthesis of 5-Substituted Hexahydro-1H-1, 4-Diazepine Analogues  

Synthesis of 5-Substituted Hexahydro-1H-1, 4-Diazepine Analogues

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作  者:Jing Shan SHEN Li Jun LEI Hai Fang MAO Jian Feng LI Ru Yun JI 

机构地区:[1]Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 200031 [2]Shanghai Jahwa Fine Chemicals Co.Ltd,Shanghai 200040

出  处:《Chinese Chemical Letters》2001年第11期951-954,共4页中国化学快报(英文版)

摘  要:5-Substituted hexahydro-1H-1,4-diazepine analogues were synthesized starting from N,N'-dibenzyl-1, 2-ethylenediamine and methyl 2, 4-dibromide butyrate through nucleophilic substitution, reduction, chlorination, debenzylation and amidation. Bioactivity tests showed that 9a had the highest agonist activity.5-Substituted hexahydro-1H-1,4-diazepine analogues were synthesized starting from N,N'-dibenzyl-1, 2-ethylenediamine and methyl 2, 4-dibromide butyrate through nucleophilic substitution, reduction, chlorination, debenzylation and amidation. Bioactivity tests showed that 9a had the highest agonist activity.

关 键 词:5-substituted hexahydro-1H-1 4-diazepine analogues synthesis bioactivity 

分 类 号:O621[理学—有机化学]

 

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