Department of Organic Chemistry Ugo Schiff, Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles (HeteroBioLab), University of Florence, Via della Lastruccia 13, I-50019 Sesto Fiorentino, Italy.
Nat Chem. 2009 Jul;1(4):269-75. doi: 10.1038/nchem.256. Epub 2009 Jun 22.
The 1,2-diamine motif is present in a number of natural products with interesting biological activity and in many important pharmaceutical agents. Chiral 1,2-diamines are also widely used as the control elements in asymmetric synthesis and catalysis. Such compounds are thus an attractive target for the synthetic chemist. Although the diamination of an alkene seems an obvious route to these structures, far less research has been devoted to it than to the analogous dihydroxylation or aminohydroxylation reactions that are well-established processes in asymmetric synthesis. Here, we examine recent advances in metal-catalysed diamination reactions and their asymmetric variants. Given the prevalence of these structures, it seems likely that they will find extensive application in the construction of natural products and drug molecules in the near future.
1,2-二胺基是许多具有有趣生物活性的天然产物和许多重要药物的特征结构。手性 1,2-二胺也是不对称合成和催化中作为控制元件的广泛应用。因此，这些化合物是合成化学家的一个有吸引力的目标。尽管烯烃的二胺化似乎是这些结构的一个明显途径，但与已确立的不对称合成中类似的二羟化或氨羟化反应相比，对其的研究要少得多。在这里，我们研究了金属催化的二胺化反应及其不对称变体的最新进展。鉴于这些结构的普遍性，它们很可能在不久的将来在天然产物和药物分子的构建中得到广泛应用。
