艾司洛尔类似物PAC的合成

Synthesis of PAC - esmolol analogue

目的研究β1-受体阻滞剂PAC的合成。方法以艾司洛尔为起始原料,羟基、胺基保护后,水解后得到的羧酸与十六醇成酯,再将羟基及胺基的保护基团脱去共6步反应得到PAC。结果与结论经六步反应得到PAC,产物经1H-NMR、13C-NMR及MS确认,总收率为13.9%。

Objective To study the synthesis of PAC, the β1-adrenoreceptor inhibitor. Methods PAC was synthesized from esmolol as starting material via six steps： protection for hydroxy and amino group, hydrolysis, esterification and de-protection of the hydroxy and amino group. Results and conclusion The structure of desired compound was confirmed by 1H-NMR , 13C-NMR and MS. The total yield was 13.9%.