A novel solid-phase synthesis of highly diverse guanidines:: Reactions of primary amines attached to the T2*linker
A novel solid-phase synthesis of highly diverse guanidines:: Reactions of primary amines attached to the T2*linker
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DOI：
10.1021/ol006440c
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发表时间：
2000-11-16
期刊：
影响因子：
5.2
通讯作者：
Bräse, S
中科院分区：
文献类型：
--
作者：
Dahmen, S;Bräse, S
[图表]伯胺与 T2* 重氮树脂的反应生成聚合物结合的三氮烯，而三氮烯又可以通过添加异硫氰酸酯进行酰化。在氧化汞(II)、甲苯磺酰氯或硝酸银存在下，通过与胺反应，形成的硫脲很容易转化为相应的胍。该反应序列提供了可能有用的药效团的三取代胍。
[GRAPHICS]The reaction of primary amines with the T2* diazonium resin generates polymer-bound triazenes, which can in turn be acylated by the addition of isothiocyanate. The formed thioureas are readily transformed into the corresponding guanidines by the reaction with amines in the presence of mercury(II) oxide, tosyl chloride, or silver nitrate. This reaction sequence furnishes trisubstituted guanidines that are potentially useful pharmacophores.