基质金属蛋白酶抑制剂伊洛马司他的合成  

Synthesis of ilomastat as a matrix metalloproteinase inhibitor

作　　者：李杰[1] 韩寒[1] 刘克良[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国新药杂志》2007年第4期300-303,共4页Chinese Journal of New Drugs

摘　　要：目的:合成基质金属蛋白酶抑制剂伊洛马司他。方法:以色氨酸甲酯盐酸盐和异己酰氯为起始原料,经过取代和缩合等7步反应得到目标化合物。结果:总产率为11.9%,结构经核磁共振氢谱和质谱验证。结论:与文献相比,本法简化了操作,缩短了反应时间,提高了收率。Objective： To synthesize ilomastat, a matrix metalloproteinase inhibitor. Methods： Starting from isohexanoyl chloride and methyl tryptophan ester hydrochloride, ilomastat was obtained via 7 reaction steps including substitution and condensation. Results ：Total yield of ilomastat was 11.9%. The structure was confirmed by ^1 H-NMR and MS. Conclusion ： The simplified synthetic procedure for ilomastat was attainable.

关 键 词：伊洛马司他 基质金属蛋白酶抑制剂 药物合成 

分 类 号：R977.3[医药卫生—药品] R914.5[医药卫生—药学]