Strategies for Large-Scale Synthesis of Coelenterazine for in Vivo Applications

被引：9
|
作者：
Shrestha, Tej B. [1 ,2 ]
Troyer, Deryl L. [2 ]
Bossmann, Stefan H. [1 ]
机构：
[1] Kansas State Univ, Dept Chem, Manhattan, KS 66506 USA
[2] Kansas State Univ, Manhattan, KS 66506 USA
来源：
SYNTHESIS-STUTTGART | 2014年 / 46卷 / 05期
基金：
美国国家科学基金会;
关键词：
palladium; zinc; organometallic reagents; Grignard reaction; regioselectivity; Negishi coupling; RENILLA-RENIFORMIS; HIGHLY EFFICIENT; BIOLUMINESCENCE; CATALYST; ALKYL; LUMINESCENCE; PYRAZINES; PROTEINS; REAGENTS; ALCOHOLS;
D O I：
10.1055/s-0033-1340556
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A new application of two Negishi-type coupling reactions for the synthesis of coelenterazine is reported. The synthesis of coelenterazine in high purity on a gram scale will enable numerous approaches to bioluminescence imaging and possibly photodynamic therapy of deep-seated tumors. Coelenterazine is the substrate for several luciferases, among them Gaussia luciferase (gLuc). This synthesis starts with pyrazin-2-amine and uses inexpensive starting materials and catalysts.
引用
收藏
页码：646 / 652
页数：7
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