申请人:RAINES Ronald Thaddeus
公开号:US20130203974A1
公开(公告)日:2013-08-08
A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diaz-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compound and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.
一种制备重氮化合物、其重氮盐和这些化合物的其他保护形式的方法。通过将带有反应性羰基基团的三级膦试剂与叠氮化物反应来制备重氮化合物。该反应也可以生成酰基三氮烯,可以通过热转化或加入碱来形成重氮化合物,或者可以分离出酰基三氮烯。该方法特别适用于将带有一个或多个电子提取基团的叠氮化合物转化为重氮化合物。该方法可以在温和条件下在水介质中进行,特别适用于在生理条件下将叠氮糖转化为重氮化合物和其重氮盐。提供了三级膦试剂,特别是那些水溶性的试剂和制备试剂的前体。