节点文献
乙酰-DL-环己基甘氨酸的合成
Synthesis of Acetyl-DL-cyclohexylglycine
【摘要】 以环己基溴为原料 ,在醇钠存在下 ,经过与丙二酸二乙酯发生烃化反应 ,再水解、酸化、脱羧制得环己基乙酸 ;后者再经溴化、氨解得到 DL-环己基甘氨酸 ;最后在醋酐存在下发生乙酰化反应得到了环氧合酶 -2(COX-2 )抑制剂 JTE-52 2的重要中间体乙酰 -DL-环己基甘氨酸。目标产物结构经元素分析 ,IR和1 H NMR验证
【Abstract】 Starting from cyclohexyl bromide, the cyclohexylacetic acid([ST5HZ]4) was obtained via condensation with diethyl malonate by means of sodium alcoholate, hydrolysis, acidification and decarboxylation. The bromination and aminolysis of [ST5HZ](4)[ST5BZ] afforded the DL cyclohexyl glycine, which was acetylated with acetic anhydride in acetic acid, giving the acetyl DL cyclohexyl glycine, a important intermediate of a COX 2 selective inhibitor, JTE 522. The target molecules structure has been characterized by element analysis,IR and NMR.
【Key words】 acetyl DL cycloxyl; glycine; JTE 522; bromide; acetic acid; diethyl malonate; synthesis;
- 【文献出处】 合成化学 ,Chinese Journal of Synthetic Chemistry , 编辑部邮箱 ,2001年03期
- 【分类号】O624
- 【被引频次】4
- 【下载频次】129