FREMSTILLING AF 2,6-DIOXOPIPERIDINDERIVATER

摘要

3-Alkyl- or fluoroalkyl-3-(4-pyridyl)piperidine-2,6- diones which can be used for treating breast cancer and which have the formula <IMAGE> in which R is an alkyl group having 2-10 carbon atoms or a fluoroalkyl group having 2-5 carbon atoms, and A is hydrogen or an alkyl group having 1-4 carbon atoms, are prepared by reacting a 4-pyridyl acetate with an alkyl or fluoroalkyl iodide, chloride or bromide in the presence of a sterically voluminous base and reacting this product with acrylamide in the presence of a sodium or potassium alkoxide having a branched chain. Potassium tert-butoxide is preferably used during both steps, and the two steps are carried out in succession at room temperature in an alcoholic or polar, aprotic solvent in a single reaction vessel.