In one aspect, the invention provides a solid catalyst comprising an active alumina catalyst impregnated with a metal hydroxide. In another aspect, the invention provides a process for preparing the inventive alumina catalyst. In certain embodiments, the catalyst may be used for the protection of amines, alcohols and thiols with a wide variety of protecting agents. This procedure is widely applicable for N-protection of amino acids which finds wide industrial applications. The catalyst is also useful for carrying out nucleophilic substitutions of aromatic halides containing an electron-withdrawing group. A wide variety of nucleophiles chosen from amines, primary and secondary, aromatic and aliphatic, as well as alcohols and thiols have been successfully employed. The methodology involves simple techniques and easy work up procedures and is thus useful for large-scale industrial preparations. Additionally, the reactions avoid the use of harmful solvents and thus satisfy the need for green chemistry.
本发明提供了一种固体催化剂,其包括用
金属氢氧化物浸渍的活性氧化铝催化剂。另外,本发明还提供了制备创新氧化铝催化剂的方法。在某些实施例中,该催化剂可用于使用各种保护剂保护胺、醇和
硫醇。这种程序广泛适用于
氨基酸的N-保护,其在工业上有广泛应用。该催化剂还可用于进行含有电子吸引基团的芳香卤代物的亲核取代。已成功地使用了各种亲核试剂,包括一级和二级芳香族和脂肪族胺、醇和
硫醇。该方法涉及简单的技术和易于操作的程序,因此对于大规模工业制备非常有用。此外,反应避免使用有害的溶剂,因此满足绿色
化学的需要。