[EN] NOVEL PROTECTING REAGENTS, PROTECTING GROUPS AND METHODS OF FORMING AND USING THE SAME<br/>[FR] NOUVEAUX REACTIFS DE PROTECTION, GROUPES DE PROTECTION, ET METHODES DE FORMATION ET D'UTILISATION DESDITS REACTIFS ET GROUPES
申请人:UNIV MISSISSIPI
公开号:WO2005100329A1
公开(公告)日:2005-10-27
New protecting reagents are provided that allow for the selective placement of a new protecting group onto a reactive site of a multifunctional compound. The reagents are 2, 3, and 4-trialkylsilylxylyl, triarylsilylxylyl or a combination of alkyl-aryl silylxylyl reagents (TIX reagents), which carry a TIX protecting group for protecting alcohols as ethers, urethanes, carbonates, acetals; amines as carbamates or ureas; and thiols as ethers or esters. The invention also provides methods of forming the 2, 3, and 4-TIX reagents; introducing the TIX protecting groups to molecules bearing hydroxyl groups, amine groups, or thiol groups; methods of removing the TIX protecting groups; and intermediate compounds formed during any one of these methods. The invention further provides methods useful in producing epothilones and analogs and derivatives thereof.
提供了一种新的保护试剂,它允许将一个新的保护基团选择性地放置在多功能化合物的反应位点上。这些试剂是2、3和4-三烷基硅氧基苄基,三芳基硅氧基苄基或烷基-芳基硅氧基苄基试剂(TIX试剂)的组合,它们带有TIX保护基团,用于将醇作为醚、尿烷、碳酸酯、缩醛进行保护;将胺作为碳酸酰胺或尿素进行保护;以及将硫醇作为醚或酯进行保护。本发明还提供了形成2、3和4-TIX试剂的方法;将TIX保护基团引入带有羟基、胺基或巯基的分子中的方法;移除TIX保护基团的方法;以及在这些方法中的任一步骤形成的中间化合物。本发明进一步提供了用于生产epothilones及其类似物和衍生物的有用方法。