手性伯胺催化Biginelli反应合成手性嘧啶酮化合物的影响因素研究

The Influencing Factors on the Synthesis of Chiral Pyrimidine Sulfo-Benzophenone Compounds Catalyzed by Chiral Primary Amine-Based Organocatalyst in Biginelli Reaction

手性嘧啶酮类化合物具有重要的药理活性应用.采用手性伯胺与金属盐的复合催化体系催化Bigi-nelli反应,可以得到高立体选择性的手性嘧啶酮化合物.通过对各种反应条件的考察,结果表明,在NbCl5与QN-NH2的协同催化作用下得到较为理想的e.e.值(69%)和产率(74%).

Chiral pyrimidine ketone compounds have important pharmacological activities and broad applications in many fields. Chiral pyrimidine sulfo-benzophenone compounds with high enantioselectivity were obtained by the Biginelli reaction, which was catalyzed by chiral primary amine and metal salt. The results show that e. e. can be up to 69 % and yield can be up to 76 % under the influence of synergistic catalysis of NbCIs and QN NHz.