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1,3-二胺是天然产物和药物的重要结构单元,相对于1,2-二胺类化合物,1,3-二胺的合成较为困难.因此,1,3-二胺的高效合成一直是有机合成领域中具有挑战的课题之一.中国科学院兰州化学物理研究所黄汉民等利用他们先前发现胺缩醛对Pd(0)氧化加成生成三元环钯“Pd-CH2NR2”亲核试剂的新型基元反应,在[Pd(Xantphos)(CH2NBn2)]OTf催化下,以100%的原子经济性实现了联烯的双官能化反应,一步合成了具有重要生理活性的药物中间体1,3-二胺.
1,3-diamine is an important structural unit of natural products and pharmaceuticals, and the synthesis of 1,3-diamine is more difficult than that of 1,2-diamines. Therefore, the efficient synthesis of 1,3-diamine has been Is one of the challenging topics in the field of organic synthesis.Huang Han-min, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, and other researchers previously used their previous discovery that the oxidation of Pd (0) by amine acetal leads to the formation of three-membered ring palladium “Pd-CH2NR2” A novel elementary reaction of nucleophiles was achieved by the Pd (Xantphos) (CH2NBn2)] OTf catalysis and the bifunctionalization of alkene was achieved with 100% atomic economy. One step synthesis of pharmaceutical intermediates with important physiological activity 1,3-diamine.