摘要
改进了Ａｓｉａｍ的萘丁美酮（１）合成法，以２－甲氧基萘计算，总收率８２％。其中２的萘环５位溴原子的脱除和４侧链碳－碳双键的氢化还原均采用高选择性的钯炭／甲酸铵催化氢转移反应。以在原应生成的二（三苯膦）二氯化钯催化偶联反应，并免用价昂的Ｎ－甲基吡咯烷酮。
Nabumetone was synthesized in 82% overall yield from 2-methoxynaphthalene according to the Asiam's method with some modifications.The 5-bromo substituent of 2 and C=C double bond of 4 were highly selectively removed and hydrogenated by a Pd-C/HCOONH_4 reduction system respectively.The (Ph_3P)_2 PdCl_2 formed in situ from PdCl_2 and Ph_3P catalyzed effectively the coupling of 3 with 3-buten-2-one in dimethylformamide.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1994年第2期49-50,57,共3页
Chinese Journal of Pharmaceuticals
关键词
萘丁美酮
钯
催化
偶联反应
合成
nabumetone, palladium catalyzed coupling reaction, catalytic transfer hydrogenation, synthesis
