METHOD FOR PRODUCING PIPERIDINE-4,4-DICARBOXYLIC ACID ESTERS Russian patent published in 2022 - IPC C07D211/62 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing esters of piperidine-4,4-dicarboxylic acids of general formula (I), R¹, R²=H, C₁-C₄-alkyl, benzyl, aryl, CH₂CH₂CO₂Alk; R³=H, C₁-C₄-alkyl, R⁴=C₁-C₄-alkyl, or salts thereof, consisting in the fact that the corresponding esters of 2-(oxyminoalkyl)malonates of general formula (II), where R¹ and R⁴ have the above values, are treated with corresponding N,N-bis(siloxy)enamines of general formula (III), where R² and R³ have the above values, in the presence of a nitrogenous base at a low temperature in an aprotic solvent, and obtained 2,2-bis(oxyminoalkyl)malonates of general formula (IV), where R¹, R², R³ and R⁴ have the above values, hydrogenated with hydrogen at high temperature and high pressure of hydrogen in the presence of a metal catalyst in the medium of a low-molecular weight alcohol with subsequent extraction of end product in free form or optionally in form of salt.

EFFECT: creation of effective and universal method of obtaining compounds of general formula I, which are applicable as key intermediate products in synthesis of pharmacologically active substances for treating such diseases as cancer, multiple sclerosis, AIDS, cardiovascular diseases, et cetera, wherein the method does not require use of additional steps of setting and removing protective groups on the nitrogen atom of the piperidine ring.

7 cl, 10 ex