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

作　　者：廖祥伟[1] 吴晓峰[1] 葛大伦[1] 程永浩[1] 吴松[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所,北京100050

出　　处：《中国新药杂志》2006年第12期990-992,共3页Chinese Journal of New Drugs

摘　　要：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.

关 键 词：N-羟乙基-2-(3'-硝基联苯基-4-亚甲磺酰基)乙酰胺 PDE3B选择性抑制剂 药物合成 

分 类 号：R914.5[医药卫生—药物化学] R977.3[医药卫生—药学]