Synthesis of [thiazolium-2,2′-14C2]-SAR97276A from [14C]-thiourea

被引:2
作者
Herbert, John M. [1 ]
Le Strat, Franck [1 ]
Oumeddour, Delphine G. [1 ]
Passey, Stephen C. [1 ]
Taylor, Keith [1 ]
Whitehead, David M. [1 ]
机构
[1] Sanofi Aventis, Dept Isotope Chem & Metabolite Synth, Alnwick Res Ctr, Alnwick NE66 2JH, Northd, England
关键词
antimalarial; carbon-14; thiazole; C-14]-sulfurol; C-14]-thiourea;
D O I
10.1002/jlcr.1816
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
[thiazolium-2,2'-C-14(2)]-SAR97276A, a bis(thiazolium) antimalarial development candidate, was synthesized from [C-14]-thiourea with an overall radiochemical yield of 15%. The synthetic route involves a modified procedure for the synthesis of [C-14]-sulfurol, also a key intermediate in thiamine synthesis, which was developed due to unlabelled chemistry proving irreproducible with the radiolabelled substrate.
引用
收藏
页码:89 / 92
页数:4
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