申请人:John Wyeth and Brother Limited
公开号:US04387230A1
公开(公告)日:1983-06-07
Dihydropyridines of formula ##STR1## where R.sup.6 is lower alkyl and R.sup.5 is lower alkyl or aryl (lower)alkyl are prepared by a novel process from sodium or potassium salts of 1-substituted-1,6-dihydro-5-hydroxy-3[2H]-pyridones. The dihydropyridines are useful as intermediates for pharmacologically active 1-optionally substituted-3-phenyl or substituted phenylpiperidin-5-ols and esters. Some of the piperidinols and esters are novel; those where the 1-substituent is aryl(lower)alkyl are intermediates, those where the 1-substituent is cycloalkyl(lower)alkyl are analgesics or antidepressants and those in which the 1-position is unsubstituted are anti-secretory agents.
公式 ##STR1## 中,R.sup.6 为低碳基,R.sup.5 为低碳基或芳基(低)碳基的二氢吡啶可通过一种新的方法从1-取代-1,6-二氢-5-羟基-3[2H]-吡啶酮的钠或钾盐制备而成。这些二氢吡啶可用作药理活性的1-可选取代-3-苯基或取代苯基哌啶-5-醇和酯的中间体。其中一些哌啶醇和酯是新颖的;其中1-取代基为芳基(低)碳基的是中间体,1-取代基为环烷基(低)碳基的是镇痛剂或抗抑郁剂,而1-位置未取代的是抗分泌剂。