Ru(Ⅱ)-BINAP型手性催化剂的合成

在国内外原有Ru(Ⅱ) BINAP合成工艺的基础上,对其起始原料和关键步骤进行了改进。以经过拆分后的联萘酚为起始原料,通过酯化反应,偶联反应和络合反应等3步反应合成了一种新型的手性催化剂,总收率达到74%。其中在合成BINAP这一关键步骤中,选用了更为易得的NiCl2·(PPh3)2作为催化剂,并对关键的后处理工作做了改进,此步反应进行平稳且收率达到90%。

Synthesis of a New Ru(Ⅱ)-BINAP Chiral Catalyst

On the basis of earlier synthetic routes of Ru(Ⅱ)-BINAP,the starting raw material was changed and the crucial steps were improved.Using 1,1′-binaphthol after resolution as starting material,a new chiral reagent was synthesized.The whole work was made up of 3 steps of ester condensation,coupling reaction and complexation reaction,and the over-all yield reached 74%.Instead of using NiCl2·(DPPE)2 as catalyst,the coupling reaction was conducted by NiCl2·(PPh3)2,which is more accessible.The yield in this step reached 90% and the reaction ran smoothly.