Direct reductive alkylation of amino acids: Synthesis of bifunctional chelates for nuclear imaging

被引:51
作者
Levadala, MK
Banerjee, SR
Maresca, KP
Babich, JW
Zubieta, J [1 ]
机构
[1] Syracuse Univ, Dept Chem, Syracuse, NY 13244 USA
[2] Mol Insight Pharmaceut Inc, Cambridge, MA 02142 USA
来源
SYNTHESIS-STUTTGART | 2004年 / 11期
关键词
reductive alkylation; amino acids; bifunctional chelators; radiopharmaceuticals; sodium triacetoxyborohydride;
D O I
10.1055/s-2004-829120
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A family of effective bifunctional chelators for technetium- and rhenium-based radiopharmaceuticals was conveniently synthesized in high yields through direct reductive N-alkylations of amino acids and their analogues with aldehydes, using NaBH(OAc)(3) as an efficient reagent. The mono-, di-, tetra- and even mixed alkylated amino acid derivatives were all prepared in one-pot synthesis.
引用
收藏
页码:1759 / 1766
页数:8
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