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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.
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页码:89 / 92
页数:4
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