作者:Robert Weis、Andreas J Kungl、Werner Seebacher
DOI:10.1016/s0040-4020(03)00072-3
日期:2003.2
1-Unsubstituted 4-dimethylamino-5,6-dihydropyridine-2(1H)-thiones were converted to isomeric piperidin-4-ols which were separated and N-methylated to 2-substituted 1-methylpiperidin-4-ols. Their 1-phenyl analogues were prepared from 4-dimethylamino-5,6-dihydro-1-phenylpyridine-2(1H)-thiones. After their conversion to dihydro-1-phenylpyridin-4(1H)-ones the hydrogenation gave isomeric 1-phenylpiperidin-4-ols
将1-未取代的4-二甲基氨基-5,6-二氢吡啶-2(1 H)-硫酮转化为异构体哌啶-4-醇,将其分离并N-甲基化为2-取代的1-甲基哌啶-4-醇。它们的1-苯基类似物由4-二甲基氨基-5,6-二氢-1-苯基吡啶-2(1 H)-硫酮制备。将它们转化为二氢-1-苯基吡啶-4(1 H)-后,氢化得到异构的1-苯基哌啶-4-醇,将其分离。通过各种方法对1-取代的哌啶-4-醇进行O-烷基化,得到二苯基吡啉的2-取代的类似物。检查了它们的抗分枝杆菌活性。通过NMR光谱研究哌啶衍生物的构型和构象。