A simple one-pot procedure for the iminium salt formation:: an efficient route to β-aryiethylamines

被引:8
|
作者
Ku, YY [1 ]
Grieme, T [1 ]
Pu, YM [1 ]
Bhatia, AV [1 ]
King, SA [1 ]
机构
[1] Abbott Labs, Global Pharmaceut Res & Dev, Chem Proc Res & Dev, N Chicago, IL 60064 USA
关键词
beta-Arylethylamines; iminium salt; Mannich reaction;
D O I
10.1016/j.tetlet.2005.01.027
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A practical and highly efficient process for the preparation of beta-arylethylamines 7 was developed. Benzylic organozinc compounds 10 were reacted with the iminium salts 9 generated in situ from the amine salt 8 and para formaldehyde in one pot and in a polar and aprotic solvent, such as NMP. A variety of the beta-arylethylamines were prepared in 43-91% yields. (C) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1471 / 1474
页数:4
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