Iminomalonate as a convenient electrophilic amination reagent for Grignard reagents
Iminomalonate as a convenient electrophilic amination reagent for Grignard reagents
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DOI：
10.1246/bcsj.75.1819
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发表时间：
2002-08-01
影响因子：
4
通讯作者：
Shimizu, M
中科院分区：
文献类型：
--
作者：
Niwa, Y;Takayama, K;Shimizu, M
2-[N-（对甲氧苯基）亚氨基]丙二酸二乙酯与烷基格氏试剂进行胺化反应，得到N-烷基化产物，产率较高。所得N-烷基化产物通过氧化除去丙二酸酯部分容易地转化为N-烷基-p-茴香胺。随后将对甲氧基苯基脱保护，得到伯胺。
Diethyl 2-[N-(p-methoxyphenyl)imino]malonate underwent amination reactions with alkyl Grignard reagents to give N-aklylation products in good yields. The obtained N-alkylation products were readily converted into N-alkyl-p-anisidines by the oxidative removal of the malonate moiety. The p-methoxyphenyl group was subsequently deprotected to give primary amines.