申请人:Gist-Brocades N.V.
公开号:US04400509A1
公开(公告)日:1983-08-23
An improved process for the trimethylsilylation of organic compounds with at least one active hydrogen atom with hexamethyldisilazane, the improvement comprising effecting the reaction in the presence of 0.001 to 10 mole percent of a catalyst of the formula X--NH--Y I wherein X and Y are individually an electron-withdrawing group or when X is an electron-withdrawing group, Y is selected from the group consisting of hydrogen and trialkylsilyl of 1 to 6 carbon atoms or X and Y together with the nitrogen atom to which they are attached form a cyclic electron-withdrawing group and novel trimethylsilylated thiols of the formula ##STR1## wherein R is a 5-or 6-membered heterocycle having at least one nitrogen or sulfur heteroatom and optionally substituted with at least one member of the group consisting of alkyl of 1 to 6 carbon atoms, phenyl, trimethylsilyl, trimethylsilyloxycarbonylmethyl and alkylamino of 1 to 6 carbon atoms, and novel trimethylsilylated 3'-substituted cephalosporanic acid derivatives.
使用六甲基二硅氨基对至少含有一个活性氢原子的有机化合物进行三甲基硅基化的改进方法,其中改进包括在0.001到10摩尔%的催化剂存在下进行反应,所述催化剂的公式为X-NH-Y I,其中X和Y分别是电子吸引基团,或当X是电子吸引基团时,Y选自由1至6个碳原子的三烷基硅基或X和Y与它们附着的氮原子一起形成环状电子吸引基团;以及具有以下公式的新型三甲基硅基化硫醇:##STR1## 其中R是至少含有一个氮或硫杂原子的5或6成员杂环,并且可选择地被1至6个碳原子的烷基,苯基,三甲基硅基,三甲基硅氧羰基甲基和1至6个碳原子的烷基氨基中的一个成员取代,以及新型的三甲基硅基化3'-取代头孢菌素酸衍生物。