UK-78282的合成

Synthesis of UK-78282

对甲氧基肉桂酸经LiAlH4还原、溴代得到3-(4-甲氧基苯基)溴丙烷,与4-哌啶甲酸乙酯反应得到的1-[3-(4-甲氧基苯基)丙基]哌啶-4-甲酸乙酯经还原后与二苯甲醇醚化,得到钾离子通道阻断剂UK-78282,总收率58%。

UK-78282, a novel potassium channels blocker, was synthesized from 4-methoxycinnamic acid by reduction and bromination to give3-(4-methoxyphenyl)bromopropane, which subjected to condensation with ethylpiperi- dine-4-carboxylate followed by reduction and etherification by diphenylmethanol with an overall yield of 58%.