N-羟乙基-2-(3′-硝基联苯基-4-亚甲磺酰基)乙酰胺的合成

Synthesis of N-(2-hydroxyethyl)-2-(3′-nitro-biphenyl-4-ylmethanesulfonyl)-acetamide

目的:合成磷酸二酯酶3B(PDE3B)选择性抑制剂N-羟乙基-2-(3′-硝基联苯基-4-亚甲磺酰基)乙酰胺。方法:以对溴苄溴为初始原料经Williamson成醚反应、氧化、酰化和Suzuki偶联4步反应合成了目标化合物。结果:目标产物的结构经核磁共振氢谱、碳谱、质谱及红外光谱等确证,4步反应的总收率为24．8%。结论:该合成路线原料易得,操作简便,可用于放大制备。

Objective ： To synthesize the selective PDE3 B inhibitor N- （2-hydroxyethyl）-2-（3 ＇-nitro-biphenyl-4-ylmethanesulfonyl）-acetamide. Methods： Starting from 4-bromobenzyl bromide, the target compound was synthesized via Williamson reaction, oxidation, acylation and Suzuki cross-coupling reaction. Results： Total yield was 24.8%. The structure of the target compound was confirmed by 1H-NMR, ^13C-NMR, MS and IR. Conclusion： The easily manipulated process to synthesize the target compound is warranted for the further pilot manufacture.