Han Zhi-Yong, Xiao Han, Gong Liu-Zhu
Hefei National Laboratory for Physical Sciences at the Microscale, Department of Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, China.
Bioorg Med Chem Lett. 2009 Jul 15;19(14):3729-32. doi: 10.1016/j.bmcl.2009.05.039. Epub 2009 May 18.
Dynamic kinetic Transfer hydrogenation reaction of 2-methyl-2,4-diaryl-2,3-dihydrobenzo[b][1,4]diazepines, using phosphoric acids as catalysts and Hantzsch ester as hydride source, has been studied. A 3,3'-H8-binol derived phosphoric acid has been identified the optimal chiral catalyst for this transformation, affording 1,3-diamine derivatives with up to 8/1 dr, 86% ee and 94% ee for the major and minor diastereomers, respectively.
以磷酸为催化剂、汉斯酯为氢化物源，对2-甲基-2,4-二芳基-2,3-二氢苯并[b][1,4]二氮杂䓬的动态动力学转移氢化反应进行了研究。已确定一种3,3'-H8-联萘衍生的磷酸是该转化反应的最佳手性催化剂，得到的1,3-二胺衍生物的非对映体比例高达8/1，主要和次要非对映体的对映体过量分别为86%和94%。
